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Reaction Total Synthesis

  • Third year students and a master course student joined our lab.

  • Dr. Li Jing won Tohoku University Professor Fujino incentive Award for 2016. . . .

  • Prof. Hayashi was introduced in Chem-Station.
  • Asymmetric Diels–Alder Reaction of α-Substituted and β,β-Disubstituted α,β-Enals via Diarylprolinol Silyl Ether for the Construction of All-Carbon Quaternary Stereocenters

    Chem. Eur. J., 22, 1–8(DOI : 10.1002/chem.201602345)
    Yujiro Hayashi, Bojan P. Bondzic, Tatsuya Yamazaki, Yogesh Gupta, Shin Ogasawara, Tohru Taniguchi, and Kenji Monde
  • Prof. Hayashi is invited to a conference Advances in Organic Chemistry – Smolenice 2016 in Slovakia from September 4-7.
  • Our chemistry was cited at OCP
    Organocatalyzed C-C Ring Construction: The Kotsuki Synthesis of (+)-Aspidospermidine
  • Time Economical Total Synthesis of (−)-Oseltamivir

    Org. Lett.,18, 3426-3429(DOI : 10.1021/acs.orglett.6b01595)
    Yujiro Hayashi and Shin Ogasawara
    Reviewed in chemistry world
    introduced in Chemical Engineering News
  • M. course member, Etienne Gauthier, went back to France.

  • Dr. course member, Shinya Shiomi, went back to Kumamoto Univ.

  • Enantioselective Total Synthesis of RQN-18690A (18-Deoxyherboxidiene)

    Org. Lett., 18, 3382-3385(DOI : 10.1021/acs.orglett.6b01524)

    Yasunobu Matsumoto, Kazuhiro Hibino, Masahiro Yonaga, Hideaki Kakeya, and Yujiro Hayashi
  • Asymmetric Aldol Reaction of Dichloroacetaldehyde Catalyzed by Diarylprolinol

    Adv. Synth. Catal. 358, 2345-2351(DOI : 10.1002/adsc.201501111)
    Yujiro Hayashi, Daichi Nakamura, Yusuke Yasui, Kotaro Iwasaki and Hiroaki Chiba
  • Sterically Demanding Oxidative Amidation of a-Substituted Malononitriles with Amines Using O

    Angew. Chem. Int. Ed., 55,, 9060-9064(DOI : 10.1002/anie.201603399)
    Jing Li, Dr. Martin J. Lear, Prof. Dr. Yujiro Hayashi

  • Dr. course member, Shinya Shiomi, joined us from Kumamoto Univ.(for 2 month)

  • New Mr. course member, Etiene Gauthier, Hirotaka Asano, joined us.(for 4 month)

  • The DFT Calculation with NBO Analysis of E/Z Enamines Derived from a-Alkoxyaldehyde with Pyrrolidine

    Bull. Chem. Soc. Jpn., 89, 455-459 (2016)
    T. Mukaiyama, T. Uchimaru, Y. Hayashi,
  • Mechanism of Oxidative Amidation of Nitroalkanes with Oxygen and Amine Nucleophiles by Using Electrophilic Iodine

    Chem. Eur. J., 22, 5538-5542 (2016)
    Jing Li, Dr. Martin J. Lear, Prof. Dr. Eunsang Kwon, Prof. Dr. Yujiro Hayashi

  • 16O/18O Exchange of Aldehydes and Ketones caused by H218O in the Mechanistic Investigation of Organocatalyzed Michael, Mannich, and Aldol Reactions

    Chem. Eur. J., 22, 5868-5872 (2016)
    Prof. Dr. Yujiro Hayashi, Dr. Takasuke Mukaiyama, Dr. Meryem Benohoud, Dr. Nishant R. Gupta, Tsuyoshi Ono, Shunsuke Toda

  • Total Synthesis of 7,10-Epimer of the Proposed Structure of Amphidinolide N, Part II: Synthesis of C17–C29 Subunit and Completion of the Synthesis

    Chem. Eur. J., 22, 3287-3291 (2016)
    Dr. Koji Ochiai, Dr. Sankar Kuppusamy, Yusuke Yasui, Tsubasa Okano, Yasunobu Matsumoto, Dr. Nishant R. Gupta, Dr. Yohei Takahashi, Prof. Dr. Takaaki Kubota, Prof. Dr. Jun'ichi Kobayashi, Prof. Dr. Yujiro Hayashi

  • Total Synthesis of 7,10-Epimer of the Proposed Structure of Amphidinolide N, Part I: Synthesis of the C1–C13 Subunit

    Chem. Eur. J., 22, 3282-3286 (2016)
    Dr. Koji Ochiai, Dr. Sankar Kuppusamy, Yusuke Yasui, Tsubasa Okano, Yasunobu Matsumoto, Dr. Nishant R. Gupta, Dr. Yohei Takahashi, Prof. Dr. Takaaki Kubota, Prof. Dr. Jun'ichi Kobayashi, Prof. Dr. Yujiro Hayashi

  • Total synthesis of avermectin B1a revisited

    J. Antibio., 69, 31-50 (2016)
    S. Yamashita, D. Hayashi, A. Nakao, Y. Hayashi, M. Hirama,


  • Pot economy and one-pot synthesis

    Chem. Sci. , 7, 866-880 (2016)
    Yujiro Hayashi

  • One-Pot Synthesis of (S)-Baclofen via Aldol Condensation of Acetaldehyde with Diphenylprolinol Silyl Ether Mediated Asymmetric Michael Reaction as a Key Step

    Org.Lett., 18, 4-7 (2016)
    Abstracted SYNFACTS 2016, 12(3), 0220
    Yujiro Hayashi, Daisuke Sakamoto, and Daichi Okamura

  • Formal Synthesis of Ezetimibe Using a Proline-mediated, Asymmetric, Three-component Mannich Reaction

    Chem.Lett., 45, 30-32 (2016)
    Yasuharu Shimasaki, Seitaro Koshino, and Yujiro Hayashi

  • New Dr. course member,Yogesh Gupta, joined us.

    • Fresh 5 graduate students joined us.

    • Pf. Negishi visited our laboratory

    • Hayashi is invited to 4th RSC / SCI symposium on Challenges in Catalysis for Pharmaceuticals and Fine Chemicals Burlington House, London in November 5, 2014

    • Nef reaction with molecular oxygen in absence of metal additives and its mechanistic insight

      Chem. Eur. J., 20,15753-15759 (2014)
      Shigenobu Umemiya, Kentaro Nishino, Itaru Satoh, and Yujiro Hayashi

    • Asymmetric Organocatalyzed Michael Addition of Nitrometane to 2-Oxoindoline-3-ylidene acetaldehyde and Three “One-pot” Sequential Synthesis of (-)-Horsfiline and (-)-Coerulescine

      Chem. Eur. J., 20, 13583-13588 (2014)
      Takasuke Mukaiyama, Kento Ogata, Itaru Sato, and Yujiro Hayashi

    • A Theoretical and Experimental Study of the Effects of Silyl Substituents in Enantioselective Reactions Catalyzed by Diphenylprolinol Silyl Ether

      Chem. Eur. J., ASAP
      Yujiro Hayashi, Daichi Okamura, Tatsuya Yamazaki, Yasuto Ameda, Hiroaki Gotoh, Seiji Tsuzuki, Tadafumi Uchimaru, and Dieter Seebach

    • 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

      Chem. Eur. J., 38, 12072-12082 (2014)
      Yujiro Hayashi, Yuya Kawamoto, Masaki Honada, Daichi Okamura, Shigenobu Umemiya, Yuka Noguchi, Takasuke Mukaiyama, and Itaru Sato

    • Asymmetric Aldol Reaction of Formaldehyde Catalyzed by Diarylprolinol

      Chem. Lett., 43, 556-558(2014)
      Yusuke Yasui, Meryem Benohoud, Itaru Sato, and Yujiro Hayashi
      Abstracted in SYNFACTS 2014, 10(4), 0430

    • Solvent-mediated Tuning of the Regioselectivity of Intramolecular Diaryl Ether Formation: Total Synthesis of (+)-Aspercyclide C

      Chem. Lett., 43, 349-351(2014)
      Tatsuya Yoshino, Shuji Yamashita, Itaru Sato, Yujiro Hayashi, and Masahiro Hirama

    • Organocatalyst-Mediated Dehydrogenation of Aldehydes to α,β-Unsaturated Aldehydes, and Oxidative and Enantioselective Reaction of Aldehydes and Nitromethane Catalyzed by Diphenylprolinol Silyl Ether

      Adv. Synth. Catal., 355, 3661-3669 (2013)
      Yujiro Hayashi, Takahiko Itoh, and Hayato Ishikawa

    • One-Pot Synthesis of (-)-Oseltamivir and Mechanistic Insights into the Organocatalyzed Michael Reaction

      Chem. Eur. J., 19, 17789-17800 (2013)
      Takasuke Mukaiyama, Hayato Ishikawa, Hiroyuki Koshino ,and Yujiro Hayashi

    • Asymmetric Formal [3 + 2] Cycloaddition Reaction of Succinaldehyde via Diarylprolinol-mediated Domino
      Aldol-Acetalization Reaction for the Construction of Tetrahydrofuran

      Chem. Lett., 42,1294-1296 (2013).
      Yujiro Hayashi, Kentaro Nishino, and Itaru Sato

    • Diarylprolinol in an Asymmetric, Direct Cross-Aldol Reaction with Alkynyl Aldehydes

      ChemCatChem, 5, 2887-2892 (2013)
      Yujiro Hayashi, Masahiro Kojima, Yusuke Yasui, Yuta Kanda, Takasuke Mukaiyama, Hiroki Shomura, Daichi Nakamura,
      Leni Ritmaleni, and Itaru Sato

    • Stoichiometric Reactions of Enamines Derived from Diphenylprolinol Silyl Ethers with Nitro Olefins and Lessons for the Corresponding Organocatalytic Conversions ? a Survey

      Helv. Chim. Acta, 96, 799-852 (2013).
      Dieter Seebach, Xiaoyu Sun, Marc-Olivier Ebert, W. Bernd Schweizer, Nirupam Purkayastha, Albert K. Beck, Jorg Duschmale, Helma Wennemers, Takasuke Mukaiyama, Meryem Benohoud, Yujiro Hayashi and Markus Reiher

    • Asymmetric Mannich Reaction of α-Keto Imines Catalyzed by Diarylprolinol Silyl Ether

      Chem. Eur. J., 19, 7678-7681 (2013)
      Yujiro Hayashi, Daisuke Sakamoto, Hiroki Shomura and Daisuke Hashizume

    • Concise Synthesis of the Tetracyclic Framework of Azadiradione: Tandem Radical Cyclization

      Chem. Lett., 42, 220-221 (2013).
      Shuji Yamashita, Akito Naruko, Takahiro Yamada, Yujiro Hayashi, Masahiro Hirama
    • Organocatalytic 1,4-Addition Reaction of α,β-γ,δ-Diunsaturated Aldehyde versus 1,6-Addition Reaction
      ChemCatChem, 7, 959 (2012).
      Yujiro Hayashi, Daichi Okamura, Shigenobu Umemiya, and Tadafumi Uchimaru
    • Prof. Hayashi was awarded Novartis Chemistry Lectureship.
      Chem. & Eng. News, Sep. 5, 2011.
      Angew. Chem., Int. Ed., 51, 2809 (2012).
    • Diarylprolinol in an asymmetric aldol reaction of an α-alkyl-α-oxo aldehyde as an electrophile
      Chem. Commun.,48, 4570 (2012).
      Yujiro Hayashi, Yusuke Yasui, Masahiro Kojima, Tsuyoshi Kawamura and Hayato Ishikawa

    • High-Yielding Synthesis of the Anti-Influenza Neuramidase Inhibitor (-)-Oseltamivir by Three “One-Pot” Operations
      Most cited paper published in Angew. Chem. Int. Ed. from 2009 to 2010.
      Rank 4th
    • One-Pot High-Yielding Synthesis of the DPP4-Selective Inhibitor ABT-341 by a Four-Component Coupling Mediated by a Diphenylprolinol Silyl Ether was selected as a cover picture of Angew. Chem., Int. Ed.