2017 
191 Enantioselective Total Synthesis of Beraprost Using Organocatalyst
Shigenobu Umemiya, Daisuke Sakamoto, Genki Kawauchi, and Yujiro Hayashi
Org. Lett., Article ASAP
DOI: 10.1021/acs.orglett.7b00134
190 Multistep Continuous-Flow Synthesis of (–)-Oseltamivir
Ogasawara, Shin; Hayashi, Yujiro:
Synthesis, 2017, 49, 424-428.
DOI: 10.1055/s-2016-0036-1588899
2016  
189 Time Economical Total Synthesis of (-)-Oseltamivir
Yujiro Hayashi and Shin Ogasawara
Org. Lett., 2016, 18 (14), pp 3426–3429
DOI: 10.1021/acs.orglett.6b01595
188 Enantioselective Total Synthesis of RQN-18690A (18-Deoxyherboxidiene)
Yasunobu Matsumoto, Kazuhiro Hibino, Masahiro Yonaga, Hideaki Kakeya, and Yujiro Hayashi
Org. Lett., 2016, 18, 3382-3385
DOI: 10.1021/acs.orglett.6b01524
187 Asymmetric Aldol Reaction of Dichloroacetaldehyde Catalyzed by Diarylprolinol
Yujiro Hayashi, Daichi Nakamura, Yusuke Yasui, Kotaro Iwasaki andHiroaki Chiba
Adv. Synth. Catal., 2016, 358, 2345-2351
DOI: 10.1002/adsc.201501111
186 Sterically Demanding Oxidative Amidation of a-SubstitutedMalononitriles with Amines Using O2
Jing Li, Dr. Martin J. Lear, Prof. Dr. Yujiro Hayashi
Angew. Chem. Int. Ed. 2016, 55,1-6,
10.1002/anie.201603399
185 The DFT Calculation with NBO Analysis of E/Z Enamines Derived from a-Alkoxyaldehyde with Pyrrolidine
T. Mukaiyama, T. Uchimaru, Y. Hayashi
Bull. Chem. Soc. Jpn, 2016, 89, 455-459,
DOI: 10.1246/bcsj.20150382
184 16O/18O Exchange of Aldehydes and Ketones caused by H218O in the Mechanistic Investigation
of Organocatalyzed Michael, Mannich, and Aldol Reactions
Prof. Dr. Yujiro Hayashi, Dr. Takasuke Mukaiyama, Dr. Meryem Benohoud,
Dr. Nishant R. Gupta, Tsuyoshi Ono and Shunsuke Toda
Chem. Eur. J., 2016, 22, 5868-5872,
DOI: 10.1002/chem.201600280.
183 Mechanism of Oxidative Amidation of Nitroalkanes with Oxygen and Amine Nucleophiles by Using Electrophilic Iodine
Jing Li, Dr. Martin J. Lear, Prof. Dr. Eunsang Kwon, Prof. Dr. Yujiro Hayashi
Chem. Eur. J., 2016, 22, 5538-5542,
DOI: 10.1002/chem.201600540.
182 Total Synthesis of 7,10-Epimer of the Proposed Structure ofAmphidinolide N,
Part II: Synthesis of C17-C29 Subunit and Completion of the Synthesis
Koji Ochiai,Sankar Kuppusamy,Yusuke Yasui,Kenji Harada
Nishant R. Gupta,Yohei Takahashi,Takaaki Kubota,Jun’ichi Kobayashi,and Yujiro Hayashi
Chem. Eur. J., 2016, 22, 3287-3291,.
DOI: 10.1002/chem.201504675.
181 Total Synthesis of 7,10-Epimer of the Proposed Structure ofAmphidinolide N,
Part I: Synthesis of the C1-C13 Subunit
Koji Ochiai,Sankar Kuppusamy,Yusuke Yasui,Tsubasa Okano,Yasunobu Matsumoto,Nishant
R. Gupta,Yohei Takahashi,Takaaki Kubota,Jun’ichi Kobayashi,andYujiro Hayashi
Chem. Eur. J., 2016, 22, 3282-3286
DOI: 10.1002/chem.201504674.
180 Total synthesis of avermectin B1a revisited
KS. Yamashita, D. Hayashi, A. Nakao, Y. Hayashi, M. Hirama,
J. Antibio., 2016, 69, 31-50
DOI: 10.1038/ja.2015.47.
179 Pot economy and one-pot synthesis
Yujiro Hayashi,
Chem. Sci., 2016, 7, 866-880,
DOI: 10.1039/C5SC02913A.
178 One-Pot Synthesis of (S)-Baclofen via Aldol Condensation of Acetaldehyde with Diphenylprolinol Silyl Ether Mediated Asymmetric Michael Reaction as a Key Step
Yujiro Hayashi, Daisuke Sakamoto, and Daichi Okamura
Org.Lett., 2016, 18, 4-7,
DOI: 10.1021/acs.orglett.5b02839.
177 Formal Synthesis of Ezetimibe Using a Proline-mediated, Asymmetric, Three-component Mannich Reaction
Yasuharu Shimasaki, Seitaro Koshino, and Yujiro Hayashi
Chem.Lett., 2016, 45, 30-32,
DOI: 10.1246/cl.150916.
2015 
176 Oxidative Amidation of Nitroalkanes with Amine Nucleophiles using Molecular Oxygen and Iodine,
Jing Li,Prof. Dr. Martin J. Lear,Yuya Kawamoto,Dr. Shigenobu Umemiya,Alice R. Wong,Prof. Dr. Eunsang Kwon,
Prof. Dr. Itaru Sato,Prof. Dr. Yujiro Hayashi,
Angew. Chem. Int. Ed., 2015, 54,12986 –12990,
DOI: 10.1002/anie.201505192.
175 Asymmetric Aldol Reaction of Chloral Catalyzed by Diarylprolinol
Y. Hayashi, S. Watanabe, Y. Yasui, S. Umemiya
ChemCatChem, 2015, 7, 1646-1649,
DOI: 10.1002/cctc.201500282.
174 Asymmetric nitrocyclopropanation of a-substituted a,b-enals catalyzed by diphenylprolinol silyl ether
for the construction of all-carbon quaternary stereogenic centers
Y. Hayashi, T. Yamazaki, Y. Nakanishi, T. Ono, T. Taniguchi, K. Monde, T. Uchimaru
Eur. J. Org. Chem. 2015, 26, 5747-5754
DOI:10.1002/ejoc.201500838.
173 Two reaction mechanisms via iminium ion intermediates: The different reactivity between diphenylprolinol silyl ether and
trifluoromethyl-substituted diarylprolinol silyl ether,
H. Gotoh, T. Uchimaru, Y. Hayashi,
Chem. Eur. J. , 21,12337-12346,DOI: 10.1002/chem.20150326.
Selected “Hot Paper
172 Asymmetric Formal [3+2] Cycloaddition Reaction of Succinaldehyde and Nitro­alkene Catalyzed by Diphenylprolinol Silyl Ether,
S. Umemiya, Y. Hayashi,
Eur. J. Org. Chem. 2015, 20, 4320-4324 DOI:10.1002/ejoc.20150623.
171 Asymmetric Aldol Reaction of α,α-Disubstituted Acetaldehydes Catalyzed by Diphenylprolinol Silyl Ether for the Construction of
Quaternary Stereogenic Centers,
Y. Hayashi, H. Shomura, Q. Xu, M. J. Lear, I. Sato,
Eur. J. Org. Chem. 2015, 20, 4316-4319 DOI:10.1002/ejoc.20150585.
170 Total Synthesis of Limonin,
S. Yamashita, A. Naruko, Y. Nakazawa, L. Zhao, Y. Hayashi, M. Hirama,
Angew. Chem. Int. Ed., 2015, , 54, 8538 –8541, DOI: 10.1002/anie.20153794.
169 Asymmetric Organocatalyzed Epoxidation of 2-Oxoindoline-3-ylidene Acetaldehydes
T. Mukaiyama, K. Ogata, T. Ono, Y. Hayashi
ChemCatChem., 2015, 7, 155-159, DOI: 10.1002/cctc.201402811.
168 Practical Route to the Left Wing of CTX1B and Total Syntheses of CTX1B and 54-deoxyCTX1B
S. Yamashita, K. Takeuchi, T. Koyama, M. Inoue, Y. Hayashi, M. Hirama,
Chem. Eur. J., 2015, 21, 2621-2328, DOI: 10.1002/chem.201405629.
2014 
167 The Asymmetric Catalytic Mannich Reaction Catalyzed by Organocatalyst–A Personal Account–,
Yujiro Hayashi,
J. Synth. Org. Chem., Jpn., 2014, 72, 1228-1238.
166 Biomimetic Total Synthesis of Cyanosporaside Aglycons from a Single Enediyne Precursor through Site-Selective p-Benzyne
Hydrochlorination,
K. Yamada, M. J. Lear, T. Yamaguchi, S. Yamashita, I. D. Gridnev, Y. Hayashi, M. Hirama,
Angew. Chem. Int. Ed., 2014, 53, 13902-13906, DOI: 10.1002/anie.201408416.
165 Asymmetric Aldol Reaction of a-Acetoxyimino Aldehydes and its Application in the Synthesis of Substituted 1,2-Oxazine Derivatives
Y. Yasui, K. Ogata, I. Sato, Y. Hayashi,
Adv. Synth. Catal., 2014, 356, 3106–3118, DOI: 10.1002/adsc.201400294.
164 Asymmetric Organocatalyzed Michael Addition of Nitrometane to 2-Oxoindoline-3-ylidene acetaldehyde and Three “One-pot” Sequential Synthesis of (–)-Horsfiline and (–)-Coerulescine
T. Mukaiyama, K. Ogata, I. Sato, Y. Hayashi,
Chem. Eur. J., 2014, 20, 13583-13588, DOI: 10.1002/chem.201403932.
Inside cover picture.
163 Asymmetric Aldol Reaction of a-Acetoxyimino Aldehydes and its Application in the Synthesis of Substituted 1,2-Oxazine Derivatives
Y. Yasui, K. Ogata, I. Sato, Y. Hayashi,
Adv. Synth. Catal., 2014, 356, 3106–3118, DOI: 10.1002/adsc.201400294.
162 Asymmetric Organocatalyzed Epoxidation of 2-Oxoindoline-3-ylidene Acetaldehydes
Takasuke Mukaiyama, Kento Ogata, Tsuyoshi Ono,and Yujiro Hayashi
ChemCatChem, 2014, 7, 155-159 (2014)
161 Nef reaction with molecular oxygen in absence of metal additives and its mechanistic insight
S. Umemiya, K. Nishino, I. Satoh, Y. Hayashi
Chem. Eur. J., 2014, 20, 15753-15759 (2014)
Hot Paper
Inside cover picture.
160 Asymmetric Organocatalyzed Michael Addition of Nitrometane to 2-Oxoindoline-3-ylidene acetaldehyde and Three “One-pot” Sequential Synthesis of (-)-Horsfiline and (-)-Coerulescine
T. Mukaiyama, K. Ogata, I. Sato, Y. Hayashi
Chem. Eur. J., 2014, 20, 13583-13588 (2014)
159 A Theoretical and Experimental Study of the Effects of Silyl Substituents in Enantioselective Reactions Catalyzed by Diphenylprolinol Silyl Ether
Y. Hayashi, D. Okamura, T. Yamazaki, Y. Ameda, H. Gotoh, S. Tsuzuki, T. Uchimaru, D. Seebach
Chem. Eur. J., 2014, 20, 17077-88(2014),DOI: 10.1002/chem.201403514.
158 Diphenylprolinol Silyl Ether Catalyzed Asymmetric Michael Reaction of Nitroalkanes and β,β-Disubstituted α,β-Unsaturated Aldehydes for the Construction of All-Carbon Quaternary Stereogenic Centers
Y. Hayashi, Y. Kawamoto, M. Honada, D. Okamura, S. Umemiya, Y. Noguchi, T. Mukaiyama, and I. Sato
Chem. Eur. J., 2014, 38, 12072-12082 (2014)
157 Asymmetric Aldol Reaction of Formaldehyde Catalyzed by Diarylprolinol
Y. Yasui, M. Benohoud, Itaru. Sato, and Y. Hayashi
Chem. Lett., 2014, 43, 556-558 (2014)
Abstracted in SYNFACTS 2014, 10(4), 0430
156 Solvent-mediated Tuning of the Regioselectivity of Intramolecular Diaryl Ether Formation: Total Synthesis of (+)-Aspercyclide C
T. Yoshino, S. Yamashita, I. Sato, Y. Hayashi, and M. Hirama
Chem. Lett., 2014, 43, 349-351 (2014)
2013 
155 Organocatalyst-Mediated Dehydrogenation of Aldehydes to α,β-Unsaturated Aldehydes, and Oxidative and Enantioselective
Reaction of Aldehydes and Nitromethane Catalyzed by Diphenylprolinol Silyl Ether
Y. Hayashi, T. Itoh, and H. Ishikawa
Adv. Synth. Catal., 18, 3661-3669 (2013)
154 One-Pot Synthesis of (-)-Oseltamivir and Mechanistic Insights into the Organocatalyzed Michael Reaction
T. Mukaiyama, H. Ishikawa H. Koshino, and Y. Hayashi
Chem. Eur. J., 52, 17789-17800 (2013)
153 Remote 1,6-Stereocontrol by Iminium-mediated Organocatalytic Events
M. J. Lear, and Y. Hayashi
ChemCatChem, 5, 3499-3501 (2013)
152 Asymmetric Formal [3 + 2] Cycloaddition Reaction of Succinaldehyde via Diarylprolinol-mediated Domino
Aldol–Acetalization Reaction for the Construction of Tetrahydrofuran
Y. Hayashi, K. Nishino, and I. Sato
Chem. Lett, 42,1294-1296 (2013)
151 Diarylprolinol in an Asymmetric, Direct Cross-Aldol Reaction with Alkynyl Aldehydes
Y. Hayashi, M. Kojima, Y. Yasui, Y. Kanda, T. Mukaiyama, H. Shomura, D. Nakamura, L. Ritmaleni, and I. Sato
ChemCatChem, 5, 2887-2892 (2013).
150 Asymmetric Aldol Reaction of Glyoxal Catalyzed by Diarylprolinol
Y. Hayashi, and M. Kojima
ChemCatChem, 5, 2883-2885 (2013).
149 Stoichiometric Reactions of Enamines Derived from Diphenylprolinol Silyl Ethers with Nitro Olefins and Lessons for the
Corresponding Organocatalytic Conversions – a Survey
Dieter Seebach, Xiaoyu Sun, Marc-Olivier Ebert, W. Bernd Schweizer, Nirupam Purkayastha, Albert K. Beck, Jörg Duschmalé, Helma Wennemers, Takasuke Mukaiyama, Meryem Benohoud, Yujiro Hayashi and Markus Reiher
Helv. Chim. Acta, 96,799-852 (2013).
148 Asymmetric Mannich Reaction of α-Keto Imines Catalyzed by Diarylprolinol Silyl Ether
Y. Hayashi, D. Sakamoto, H. Shomura and D. Hashizume
Chem. Eur. J., 19,7678-7681 (2013)
147 Pot Economy in the Synthesis of Prostaglandin A1 and E1 Methyl Esters
Y. Hayashi, and S. Umemiya
Angew. Chem., Int. Ed., 52,3450-3452 (2013).
146 Concise Synthesis of the Tetracyclic Framework of Azadiradione: Tandem Radical Cyclization
S. Yamashita, A. Naruko, T. Yamada, Y. Hayashi, and M. Hirama
Chem. Lett., 42, 220-221 (2013).
145 Stereoselective synthesis of zoanthenol ABC-ring by radical strategy
S. Yamashita, N. Suda, Y. Hayashi, and M. Hirama
Tetrahedron Letters, 54, 1389 (2013).
144 Remote C-H bond functionalization of androstane C-ring: C12-amination
S. Yamashita, M. Himuro, Y. Hayashi, and M. Hirama
Tetrahedron Letters, 54, 1307 (2013).
2012 
143 Organocatalytic 1,4-Addition Reaction of α,β-γ,δ-Diunsaturated Aldehyde versus 1,6-Addition Reaction
Y. Hayashi, D. Okamura, S. Umemiya, and T. Uchimaru
ChemCatChem 4, 959 (2012).
142 Diarylprolinol in an asymmetric aldol reaction of an α-alkyl-α-oxo aldehyde as an electrophile
Y. Hayashi, Y. Yasui, M. Kojima, T. Kawamura and H. Ishikawa
Chem. Commun., 48, 4570 (2012).
2011 
141 Organocatalytic, Enantioselective Intramolecular [6 + 2] Cycloaddition Reaction for the Formation of
Tricyclopentanoids and Insight on Its Mechanism from a Computational Study
Y. Hayashi, H. Gotoh, M. Honma, K. Sankar, I. Kumar, H. Ishikawa, K. Konno, H. Yui, S. Tsuzuki, and T. Uchimaru
J. Am. Chem. Soc., 133, 20175 (2011).
140 Synthesis of (-)-Oseltamivir by Using a Microreactor in the Curtius Rearrangement
H. Ishikawa, Bojan P. Bondzic and Y. Hayashi
Eur. J. Org. Chem., 6020 (2011).
139 One-Pot Synthesis of Chiral Aziridines by a Domino Reaction by Using Desulfonylative Formation on the N-Tosyl
Imine of Chloroacetaldehyde with an Asymmetric Mannich Reaction as a Key step
Y. Hayashi, T. Urushima, D. Sakamoto, K. Torii and H. Ishikawa
Chem. Eur. J., 17, 11715 (2011).
138 Asymmetric Mannich Reaction of Imines Derived from Aliphatic and Aromatic Aldehydes Catalyzed by Diarylprolinol Silyl Ether
T. Urushima, H. Ishikawa and Y. Hayashi
Chem. Eur. J. 17, 8273 (2011).
137 Organocatalyzed Michael Addition of Aldehydes to Nitro Alkenes - Generally Accepted Mechanism Revisited and Revised.
Krystyna Patora-Komisarska, Meryem Benohoud, Hayato Ishikawa, Dieter Seebach and Yujiro Hayashi
Helvetica Chemica Acta, 94, 719 (2011).
136 Oxidative and Enantioselective Cross-Coupling of Aldehydes and Nitromethane Catalyzed by Diphenylprolinol Silyl Ether
Y. Hayashi, T. Itoh, H. Ishikawa
Angew. Chem., Int. Ed., 50, 3920 (2011).
Hot Paper
135 Asymmetric One-Pot Four-Component Coupling Reaction: Synthesis of Substituted Tetrahydropyrans Catalyzed by
Diphenylprolinol Silyl Ether
H. Ishikawa, S. Sawano, Y. Yasui, Y. Shibata and Y. Hayashi
Angew. Chem., Int. Ed., 50, 3774 (2011).
134 One-Pot Synthesis of Chiral α-Substituted β,γ-Epoxy Aldehyde Derivatives through an Asymmetric Aldol Reaction
of Chloroacetaldehyde
Y. Hayashi, Y. Yasui, T. Kawamura, M. Kojima and H. Ishikawa
Angew. Chem., Int. Ed., 50, 2804 (2011).
133 Diarylprolinol in the Direct Asymmetric Aldol Reaction of Trifluoromethylacetaldehyde Ethyl Hemiacetal with Aldehyde
Y. Hayashi, Y. Yasui, T. Kawamura, M. Kojima and H. Ishikawa
Synlett, 485, (2011).
132 One-Pot High-Yielding Synthesis of the DPP4-Selective Inhibitor ABT-341 by a Four-Component Coupling Mediated by a Diphenylprolinol Silyl Ether
H. Ishikawa, M. Honma,and Y. Hayashi
Angew. Chem.,Int. Ed., 50, 2824 (2011).
Very Important Paper
2010 
131 Asymmetric Epoxidation of α-Substituted Acroleins Catalyzed by Diphenylprolinol Silyl Ether
B. P. Bondzic, T. Urushima, H. Ishikawa, and Y. Hayashi
Org.Lett., 12, 5434 (2010).
130 High-Yielding Synthesis of the Anti-Influenza Neuraminidase Inhibitor (−)-Oseltamivir by Two “One-Pot” Sequences
H. Ishikawa, T. Suzuki, H. Orita, T. Uchimaru and Y. Hayashi
Chem. Eur. J., 16, 12616 (2010).
129 Enantio- and Diastereoselective Synthesis of Piperidines by Coupling of Four Components in a “One-Pot” Sequence
Involving Diphenylprolinol Silyl Ether Mediated Michael Reaction
T. Urushima, D. Sakamoto, H. Ishikawa, and Y. Hayashi
Org.Lett., 12, 4588 (2010).
Abstracted in SYNFACTS, 12, 1420, (2010).
128 Formal Total Synthesis of Fostriecin by 1,4-Asymmetric Induction with an Alkyne-Cobalt Complex
Y. Hayashi, H. Yamaguchi, M. Toyoshima, K. Okado, T. Toyo, M. Shoji
Chem. Eur. J., 16, 10150 (2010).
127 Polymeric Ethyl Glyoxylate in an Asymmetric Aldol Reaction Catalyzed by Diarylprolinol
T. Urushima, Y. Yasui, H. Ishikawa, and Y. Hayashi
Org.Lett., 12, 2966 (2010).
126 One-pot synthesis of chiral bicyclo[3.3.0]octatrienes using diphenylprolinol silyl ether-mediated ene-type reaction
H. Gotoh, H. Ogino, H. Ishikawa, and Y. Hayashi
Tetrahedron, 66, 4894 (2010).
125 Syntheses of Fumagillin and Ovalicin
J. Yamaguchi, and Y. Hayashi
Chem. Eur. J., 16, 3884 (2010).
2009 
124 Diphenylprolinol Silyl Ether as a Catalyst in an Asymmetric, Catalytic, and Direct Michael Reaction of Nitroethanol with α,β - Unsaturated Aldehydes
H. Gotoh, D. Okamura, H. Ishikawa, and Y. Hayashi
Org.Lett., 11, 4056 (2009).
123 Structures of the Reactive Intermediates in Organocatalysis with Diarylprolinol Ethers
Uros Groselj, Dieter Seebach, D. Michael Badine, W. Bernd Schweizer, Albert K. Beck, Ingo Krossing, Petra Klose, Yujiro Hayashi, Tadafumi Uchimaru
Helvetica Chimica Acta., 92, 1225 (2009).
122 Asymmetric Aldol Reaction of Acetaldehyde and Isatin Derivatives for the Total Syntheses of ent-Convolutamydine E and CPC-1 and a Half Fragment of Madindoline A and B
T. Itoh, H. Ishikawa, and Y. Hayashi
Org.Lett., 11, 3854 (2009).
121 Total synthesis and determination of the absolute configuration of FD-838, a naturally occurring azaspirobicyclic product
Y. Hayashi, K. Sankar, H. Ishikawa, Y. Nozawa, K. Mizoue, H. Kakeya
Bioorganic & Medicinal Chemistry Letters, 19, 3863 (2009).
120 Diphenylprolinol silyl ether as a catalyst in an asymmetric, catalytic and direct alpha - benzoyloxylation of aldehydes
H. Gotoh, Y. Hayashi
Chem. Commun, 3083 (2009).
119 Conversion of Alcohols to Alkyl Aryl Sulfides by a New Type of Oxidation-Reduction Condensation Using Phenyl Diphenylphosphinite
K. Kuroda, Y. Maruyama, Y. Hayashi, T. Mukaiyama
Bull. Chem. Soc. Jpn., 82, 381 (2009).
118 High-Yielding Synthesis of the Anti-Influenza Neuramidase Inhibitor (-)-Oseltamivir by Three "One-Pot" Operations
H. Ishikawa, T. Suzuki, Y. Hayashi
Angew. Chem. Int. Ed., 48, 1304 (2009).
Hot Paper!
Most accessed articles in 01/2009 : Ranked as 1st!
117 Diphenylprolinol Silyl Ether as a Catalyst in an Enantioselective, Catalytic Michael Reaction for the Formation of alpha,alpha- Disubstituted alpha - Amino Acid Derivatives
Y. Hayashi, K. Obi, Y. Ohta, D. Okamura, H. Ishikawa
Chem. Asian. J., 4, 246 (2009).
116 Diphenylprolinol Silyl Ether Catalysis in an Asymmetric Formal Carbo [3 + 3] Cycloaddition Reaction via a Domino Michael/Knoevenagel Condensation
Y. Hayashi, M. Toyoshima, H. Gotoh, H. Ishikawa
Org. Lett., 11, 45 (2009)
Abstracted in SYNFACTS 2009, 327
2008 
115 Asymmetric, Catalytic, and Direct Self-Aldol Reaction of Acetaldehyde Catalyzed by Diarylprolinol
Y. Hayashi, S. Samanta, T. Itoh , H. Ishikawa
Org. Lett.,10, 5581, (2008)
114 Direct Organocatalytic Mannich Reaction of Acetaldehyde: An Improved Catalyst and Mechanistic Insight from a Computational Study
Y. Hayashi, T. Okano, T. Itoh, T. Urushima, H. Ishikawa, T. Uchimaru
Angew. Chem. Int. Ed., 47, 9053 (2008).
113 Stereospecific Synthesis of sec- and tert-Alkyl Azides from Alcohols and Trimethylsilyl Azide by a New Type of Oxidation–Reduction Condensation Using Phenyl Diphenylphosphinite and Trimethylsilylmethyl Azide
T. Mukaiyama, K. Kuroda, Y. Maruyama Y. Hayashi
Chem. Lett., 37, 1072 (2008).
112 Stereospecific synthesis of alkyl aryl sulfides from alcohols and 2-sulfanylbenzothiazole using aryl diphenylphoshinite and azide compounds by a new type of oxidation-reduction condensation
K. Kuroda, Y. Maruyama, Y. Hayashi, T. Mukaiyama
Chem. Lett., 37, 836 (2008).
111 Epoxyquinol B, a Naturally Occurring Pentaketide Dimer, Inhibits NF-kB Signaling by Crosslinking TAK1
H. Kamiyama, T. Usui, H. Sakurai, M. Shoji, Y. Hayashi, H. Kakeya, H. Osada
Biosci. Biotechnol. Biochem., 72, 1894 (2008).
110 Epoxyquinol B shows antiangiogenic and antitumor effects by inhibiting VEGFR2, EGFR, FGFR, and PDGFR
H. Kamiyama, H. Kakeya, T. Usui, K. Nishikawa, M. Shoji, Y. Hayashi, H. Osada
Oncology Research, 17, 11 (2008).
109 Fungal metabolite, epoxyquinol B, crosslinks proteins by epoxy-thiol conjugation
H. Kamiyama, T. Usui, M. Uramoto, H. Takagi, M. Shoji, Y. Hayashi, H. Kakeya, H. Osada
J. Antibiotics, 61, 94 (2008).
108 The Asymmetric Total Synthesis of (+)-Cytotrienin A, an Ansamycin-Type Anticancer Drug
Yujiro Hayashi, Mitsuru Shoji, Hayato Ishikawa, Junichiro Yamaguchi, Tomohiro Tamura, Hiroki Imai,
Yosuke Nishigaya, Kenichi Takabe, Hideaki Kakeya, Hiroyuki Osada
Angew. Chem. Int. Ed., 47, 6657 (2008).
Abstracted in SYNFACTS 2009, 247
107 Asymmetric Diels-Alder Reactions of alpha,beta-Unsaturated Aldehydes Catalyzed by a Diarylprolinol Silyl Ether Salt in the Presence of Water
Yujiro Hayashi, Sampak Samanta, Hiroaki Gotoh, Hayato Ishikawa
Angew. Chem. Int. Ed., 47, 6634 (2008).
106 Preparation of Alkyl Aryl Sulfides from Alcohols and 2-Sulfanylbenzothiazole by a New Type of Oxidation–Reduction Condensation Using Aryl Diphenylphosphinite and Benzoquinone Derivatives
Kiichi Kuroda, Yujiro Hayashi, Teruaki Mukaiyama
Chem. Lett., 37, 592 (2008).
105 The Effectiveness of Proteinogenic Amino Acids in the Asymmetric Aldol Reaction in DMSO and Aqueous DMSO
Yujiro Hayashi, Takahiko Itoh, Norio Nagae, Masahiro Ohkubo, Hayato Ishikawa
Synlett, 2008, 1565.
104 Asymmetric Michael Reaction of Acetaldehyde Catalyzed by Diphenylprolinol Silyl Ether
Yujiro Hayashi, Takahiko Itoh, Masahiro Ohkubo, Hayato Ishikawa
Angew. Chem. Int. Ed., 47, 4722 (2008).
103 Diphenylprolinol Silyl Ether as a Catalyst in an Enantioselective, Catalytic, Formal Aza [3+3] Cycloaddition Reaction for the Formation of Enantioenriched Piperidines
Yujiro Hayashi, Hiroaki Gotoh, Ryouhei Masui, Hayato Ishikawa
Angew. Chem. Int. Ed., 47, 4012 (2008).
Hot Paper!
Abstracted in SYNFACTS 2008, 764
102 Formal Total Synthesis of Fostriecin via 1,4-Asymmetric Induction Using Cobalt-Alkyne Complex
Yujiro Hayashi, Hirofumi Yamaguchi, Maya Toyoshima, Kotaro Okado, Takumi Toyo, and Mitsuru Shoji
Org. Lett. 10, 1405 (2008).
Abstracted in SYNFACTS 2008, 899
101 Proline-Mediated Enantioselective Construction of Tetrahydropyrans via a Domino Aldol/Acetalization Reaction
Damien Hazelard, Hayato Ishikawa, Daisuke Hashizume, Hiroyuki Koshino, and Yujiro Hayashi
Org. Lett. 10, 1445 (2008).
Abstracted in SYNFACTS 2008, 762
100 A Diarylprolinol in an Asymmetric, Catalytic, and Direct Crossed-Aldol Reaction of Acetaldehyde
Yujiro Hayashi, Takahiko Itoh, Seiji Aratake, Hayato Ishikawa,
Angew. Chem. Int. Ed., 47, 2082 (2008).
This paper is dedicated to Prof. E. J. Corey on the occasion of his 80th birthday.
Hot Paper!
Abstracted in SYNFACTS 2008, 533
99 1,4-Asymmetric Induction using a Cobalt Alkyne Complex,
Yujiro Hayashi, Hirofumi Yamaguchi, Maya Toyoshima, Satoshi Nasu, Koji Ochiai, and Mitsuru Shoji
Organometallics, 27, 163 (2008).
98 Direct Asymmetric alpha-Amination of Cyclic Ketones Catalyzed by Siloxyproline,
Yujiro Hayashi, Seiji Aratake, Yoshinaga Imai, Kazuhiro Hibino, Qi-Yin Chen, Junichiro Yamaguchi, Tadafumi Uchimaru
Chem. Asian J. 3, 225 (2008).
This paper is dedicated to Prof. Teruaki Mukaiyama on the occasion of his 80th birthday.
97 Organic Solvent-Free, Enantio- and Diastereoselective, Direct Mannich Reaction in the Presence of Water,
Yujiro Hayashi, Tatsuya Urushima, Seiji Aratake, Tsubasa Okano, and Kazuki Obi,
Org. Lett. 10, 21 (2008).
2007 
96 Chemistry of Epoxyquinols A, B, and C and Epoxytwinol A
Mitsuru Shoji, Yujiro Hayashi European Journal of Organic Chemistry, 23, 3783 (2007)
95 Diphenylprolinol Silyl Ether as Catalyst of an Asymmetric, Catalytic, and Direct Michael Reaction of Nitroalkanes with α,β -Unsaturated Aldehydes,
Hiroaki Gotoh, Hayato Ishikawa, Yujiro Hayashi,
Org. Lett., 9, 5307 (2007).
Most-Accessed Articles: October-December, 2007 : Ranked as 15th!
94 Highly Diastereo- and Enantioselective Direct Aldol Reactions of Aldehydes and Ketones Catalyzed by Siloxyproline in the Presence of Water,
Seiji Aratake, Takahiko Itoh, Tsubasa Okano, Norio Nagae, Tatsunobu Sumiya, Mitsuru Shoji, Yujiro Hayashi,
Chem. Eur. J., 13, 10246 (2007).
93 Conversion of tertiary alcohols to tert-alkyl azides by way of quinone-mediated oxidation-reduction condensation using alkyl diphenylphosphinites, Kiichi Kuroda, Yujiro Hayashi and Teruaki Mukaiyama, Tetrahedron, 63, 6358 (2007).
92 Organocatalyst-Mediated Enantioselective Intramolecular Aldol Reaction Featuring the Rare Combination of Aldehyde as Nucleophile and Ketone as Electrophile
Y. Hayashi, H. Sekizawa, J. Yamaguchi, H. Gotoh, J. Org. Chem., 72, 6493 (2007).
Most-Accessed Articles: July-September, 2007 : Ranked as 8th!
91 Diarylprolinol Silyl Ether as Catalyst of an exo-Selective, Enantioselective Diels-Alder Reaction
H. Gotoh, Y. Hayashi,
Org. Lett., 9, 2859 (2007).
90 Diphenylprolinol Silyl Ether as a Catalyst in an Enantioselective, Catalytic, Tandem Michael/Henry Reaction for the Control of Four Stereocenters
Y. Hayashi, T. Okano, S. Aratake, D. Hazelard,
Angew. Chem. Int. Ed., 46, 4922 (2007).
89 Small organic molecule in enantioselective, direct aldol reaction in water,
S. Aratake, T. Itoh, T. Okano, T. Usui, M. Shoji and Y. Hayashi,
Chem. Commun., 2007, 2524.
88 L-Proline-catalyzed enantioselective one-pot cross-Mannich reaction of aldehydes,
Y Hayashi, T. Urushima, W. Tsuboi, M. Shoji,
Nature Protocols 2, 113-118 (01 Feb 2007) .
87 Ultracentrifuge-mediated Diels-Alder Reaction in a Two-phase System of Water and Chloroform,
Y. Hayashi, M. Takeda, M. Shoji, M. Morita, Chem. Lett., 36, 68-69 (2007).
This paper is dedicated to Prof. Teruaki Mukaiyama on the occasion of his 80th birthday.
86 Dry and Wet Prolines for Asymmetric Organic-Solvent-Free Aldehyde-Aldehyde and Aldehyde-Ketone Aldol Reactions, Y. Hayashi, S. Aratake, T. Itoh, T. Okano, T. Sumiya, M. Shoji, Chem. Commun. 2007, 957.
2006 
85 Preparation of tert-Alkyl Azides from Tertiary Alcohols by Way of Benzoquinone-mediated Oxidation-Reduction Condensation, K. Kuroda, N. Kaneko, Y. Hayashi, T. Mukaiyama, Chem. Lett., 35, 1432-1433 (2006).
84 In Water or in the Presence of Water? , Y. Hayashi, Angew. Chem. Int. Ed., 45, 8103 (2006)
83 Enantio- and Diastereoselective Total Synthesis of (+)-Panepophenanthrin, a Ubiquitin-Activating Enzyme Inhibitor, and Biological Properties of Its New Derivatives, M. Matsuzawa, H. Kakeya, J. Yamaguchi, M. Shoji, R, Onose, H. Osada, Y. Hayashi, Chem. Asian. J., 1, 845(2006).
82 Enantioselective Ene Reaction of Cyclopentadiene and ,-Enals Catalyzed by a Diphenylprolinol Silyl Ether
H. Gotoh, R. Masui, H. Ogino, M. Shoji, Y. Hayashi, Angew. Chem. Int. Ed. 45 6853 (2006).
81 Combined Proline–Surfactant Organocatalyst for the Highly Diastereo- and Enantioselective Aqueous Direct Cross-Aldol Reaction of Aldehydes, Y. Hayashi*, S. Aratake, T. Okano, J. Takahashi, T. Sumiya, M. Shoji, Angew. Chem. Int. Ed. 45, 5527(2006).
80 Large Nonlinear Effect Observed in the Enantiomeric Excess of Proline in Solution and That in the Solid State, Y. Hayashi*, M. Matsuzawa, J. Yamaguchi, S. Yonehara, Y. Matsumoto, M. Shoji, D. Hashizume, H. Koshino, Angew. Chem. Int. Ed. 45, 4593 (2006).
79 Computational Study on the Reaction Mechanism of the Key Thermal [4 + 4] Cycloaddition Reaction in the Biosynthesis of Epoxytwinol A, I. Shiina, T. Uchimaru, M. Shoji, H. Kakeya, H. Osada, and Y. Hayashi, Org. Lett., 8, 1041 (2006).
78 Highly Diastereo- and Enantioselective Direct Aldol Reactions in Water, Y. Hayashi, T. Sumiya, J. Takahashi, H. Gotoh, T. Urushima, M. Shoji, Angew. Chem. Int. Ed. 45, 958 (2006).
77 Concise Enantio- and Diastereoselective Total Syntheses of Fumagillol, RK-805, FR65814, Ovalicin, and 5-Demethylovalicin J. Yamaguchi, M. Toyoshima, M. Shoji, H. Kakeya, H. Osada, Y. Hayashi, Angew. Chem. Int. Ed., 45, 789 (2006).
2005 
76 Enantio- and Diastereoselective Total Synthesis of EI-1941-1, -2, and -3, Inhibitors of Interleukin-1 Converting Enzyme, and Biological Properties of Their Derivatives, M. Shoji, T. Uno, H. Kakeya, R. Onose, I. Shiina, H. Osada, and Y. Hayashi, J. Org. Chem., 70, 9905 (2005).
75 RKTS-33, an Epoxycyclohexenone Derivative That Specifically Inhibits Fas Ligand-Dependent Apoptosis in CTL-Mediated Cytotoxicity, T. Mitsui, Y. Miyake, H. Kakeya, Y. Hayashi, H. Osada, T. Kataoka, Biosci. Biotechnol. Biochem., 69, 1923-1928 (2005).
74 Cysteine-Derived Organocatalyst in a Highly Enantioselective Intramolecular Michael Reaction, Y. Hayashi, H. Gotoh, T. Tamura, H. Yamaguchi, R. Masui, and M. Shoj, J. Am. Chem Soc, 127, 16028 (2005).
73 The Direct, Enantioselective, One-Pot, Three-Component,Cross-Mannich Reaction of Aldehydes: The Reason for the Higher Reactivity of Aldimine versus Aldehyde in Proline-Mediated Mannich and Aldol Reactions, Y. Hayashi, T. Urushima, M. Shoji, T. Uchimaru, I. Shiina, Adv. Synth. Catal., 347, 1604 (2005).invited paper of special issue dedicated to C-C bond formation.
72 The stereoselective synthesis of α-substituted β-amino secondary alcohols based on the proline-mediated, asymmetric, three-component Mannich reaction and its application to the formal total synthesis of nikkomycins B and Bx, Y. Hayashi, T. Urushima, M. Shin and M. Shoji Tetrahedron, 48, 11393 (2005). Invited paper of the special issue dedicated to Multicomponent Reactions.
71 The First Asymmetric Total Synthesis of Synerazol, an Antifungal Antibiotic, and Determination of its Absolute Stereochemistry, Y. Hayashi, M. Shoji, T. Mukaiyama, H. Gotoh, S. Yamaguchi, M. Nakata, H. Kakeya, H. Osada, J. Org. Chem.,70, 5643 (2005).
70 Diphenylprolinol Silyl Ethers as Efficient Organocatalysts for the Asymmetric Michael Reaction of Aldehydes and Nitroalkenes, Y. Hayashi, H. Gotoh, T. Hayashi, M. Shoji, Angew. Chem. Int. Ed., 44, 4212-4215 (2005).
69 Epolactaene binds human Hsp60 Cys442 resulting in the inhibition of chaperone activity, Y. Nagumo, H. Kakeya, M. Shoji, Y. Hayashi, N. Dohmae, H. Osada, Biochem. J., 387, 835-840 (2005).
68 Determination by asymmetric total synthesis of the absolute configuration of lucilactaene, a cell cycle inhibitor in p53-transfected cells, J. Yamaguchi, H. Kakeya, T. Uno, M. Shoji, H. Osada, and Y. Hayashi, Angew. Chem. Int. Ed., 44, 3110-3115 (2005).
67 Synthesis of a- and/or g-benzoyloxy-a,b-enones from a-halo-a,b-enones, Y. Hayashi, M. Shoji, and S. Kishida, Tetrahedron Lett. 46, 681-685 (2005).
66 The Total Synthesis of Epoxyquinols A, B, C and Epoxytwinol A and the Reactivity of a 2H-Pyran Derivative as the Diene Component in the Diels-Alder Reaction, M. Shoji, H. Imai, M. Mukaida, K. Sakai, H. Kakeya, H. Osada, and Y. Hayashi, J. Org. Chem. 70, 79-91 (2005).
2004 
65 Stereoselective Total Synthesis of ent-EI-1941-2 and Epi-ent-EI-1941-2, M. Shoji, T. Uno, and Y. Hayashi, Org. Lett., 6, 4535-4538 (2004).
64 A. Highly Active 4-Siloxyproline Catalyst for Asymmetric Synthesis. Y. Hayashi, J. Yamaguchi, K. Hibino, T. Sumiya, T. Urushima, M. Shoji, D. Hashizume, and H. Koshino, Adv. Synth. Catal., 346, 1435-1439 (2004).
63 Structure-activity relationships of epolactaene derivatives: structural requirements for inhibition of Hsp60 chaperone activity, Y. Nagumo, H. Kakeya, J. Yamaguchi, T. Uno, M. Shoji, Y. Hayashi, H. Osada, Bioorg. Med. Chem. Lett., 14, 4425-4429 (2004).
62 Direct Proline-Catalyzed Asymmetric a-Aminoxylation of Aldehydes and Ketones, Y. Hayashi, J. Yamaguchi, T. Sumiya, K. Hibino, M. Shoji, J. Org. Chem. 69, 5966-5973 (2004).
61 The Chiral Diamine Mediated Asymmetric Baylis-Hillman Reaction, Y. Hayashi, T. Tamura, M. Shoji, Adv. Synth. Catal., 346, 1106-1110 (2004).
60 Application of high pressure, induced by water freezing, to the direct asymmetric aldol reaction, Y. Hayashi, W. Tsuboi, M. Shoji, N. Suzuki, Tetrhedron Lett., 45, 4353-4356 (2004).
59 Different Reaction Modes for the Oxidative Dimerization of Epoxyquinols and Epoxyquinones. Importance of Intermolecular Hydrogen-Bonding, M. Shoji, H. Imai, I. Shiina, H. Kakeya, H. Osada, Y. Hayashi, J. Org. Chem., 69, 1548-1556 (2004).
58 Direct Proline-Catalyzed Asymmetric a-Aminoxylation of Ketones, Y. Hayashi, J. Yamaguchi, T. Sumiya, M. Shoji, Angew. Chem. Int Ed., 43, 1112-1115 (2004).
2003 
57 Direct proline catalyzed asymmetric a-aminooxylation of aldehydes, Y. Hayashi, J. Yamaguchi, K. Hibino, M. Shoji, Tetrahedron Lett., 44, 8293-8296 (2003).
56 Novel Non-peptide Inhibitors Targeting Death Receptor-Mediated Apoptosis, H. Kakeya, Y. Miyake, M. Shoji, S. Kishida, Y. Hayashi, T. Kataoka, H. Osada, Bioorganic & Medical Chem. Lett., 13, 3743-3746 (2003).
55 Application of High Pressure Induced by Water-Freezing to the Direct Catalytic Asymmetric Three-Component List-Barbas-Mannich Reaction, Y. Hayashi, W. Tsuboi, M. Shoji, N. Suzuki, J. Am. Chem. Soc., 125, 11208-11209 (2003).
54 Reaction Modes of Oxidative Dimerization of Epoxycyclohexenols, M. Shoji, S. Kishida, Y. Kodera, I. Shiina, H. Kakeya, H. Osada, Y. Hayashi, Tetrahedron Lett., 44, 7205-7207 (2003).
53 The Diect and Enantioselective, One-pot, Three-Component, Cross-Mannich Reaction of Aldehydes, Y. Hayashi, W. Tsuboi, I. Ashimine, T. Urushima, M. Shoji, K. Sakai, Angew. Chem. Int. Ed., 42, 3677-3680 (2003).
52 Asymmetric Total Synthesis of Pseurotin A, Y. Hayashi, M. Shoji, S. Yamaguchi, T. Mukaiyama, J. Yamaguchi, H. Kakeya, H. Osada, Org. Lett., 5, 2287-2290 (2003).
2002 
51 A Practical Total Synthesis of Both Enantiomers of Epoxyquinols A and B, M. Shoji, S. Kishida, M. Takeda, H. Kakeya, H. Osada, and Y. Hayashi, Tetrahedron Lett., 43, 9155-9158 (2002).
50 The Baylis-Hillman Reaction under High Pressure Induced by Water-Freezing, Y. Hayashi, K. Okado, I. Ashimine, and M. Shoji, Tetrahedron Lett., 43, 8683-8686 (2002).
49 Asymmetric Total Synthesis of (-)-Azaspirene, a Novel Angiogenesis Inhibitor, Y. Hayashi, M. Shoji, J. Yamaguchi, K. Sato, S. Yamaguchi, T. Mukaiyama, K. Sakai, Y. Asami, H. Kakeya, and H. Osada, J. Am. Chem. Soc., 124, 12078-12079 (2002).
48 The Diastereoelective Asymmetric Total Synthesis of NG-391, a Neuronal Cell-Protecting Molecule, Y. Hayashi, J. Yamaguchi, and M. Shoji, Tetrahedron, 58, 9839-9846 (2002).
47 Diastereoselective Total Synthesis of Both Enantiomers of Epolactaene, Y. Hayashi, J. Kanayama, J. Yamaguchi, and M. Shoji, J. Org. Chem. 67, 9443-9448 (2002).
46 The HfCl4-Mediated Diels-Alder Reaction of Furan, Y. Hayashi, M. Nakamura, S. Nakao, T. Inoue, and M. Shoji, Angew. Chem. Int. Ed., 41, 4079-4082 (2002).
45 A Novel Adenine Nucleotide Translocase Inhibitor, MT-21, Induces Cytochrome c Release by a Mitochondrial Permeability Transition-independent Mechanism, K. Machida, Y. Hayashi, and H. Osada, J. Bio. Chem., 277, 31243-31248 (2002).
44 Total Synthesis of (+)-Epoxyquinols A and B, M. Shoji, J. Yamaguchi, H. Kakeya, H. Osada, and Y. Hayashi, Angew. Chem. Int. Ed., 41, 3192-3194 (2002).
43 b-Ketothioester as a reactive Knoevenagel donor, Y. Hayashi, Y. Miyamoto, and M. Shoji, Tetrahedron Lett., 43, 4079-4082 (2002).
42 Oxidative Double Bond Cleavage of a-Substituted Styrenes with Molecular Oxygen, Y. Hayashi, M. Takeda, Y. Miyamoto, and M. Shoji, Chem. Lett., 2002, 414-415.
41 Application of High Pressure Induced by Water-freezing to the Michael Reaction of Alcohols with a,b-Enones, Y. Hayashi, and K. Nishimura, Chem. Lett., 2002, 296-297.