Chin. J. Org. Chem. ›› 2006, Vol. 26 ›› Issue (12): 1692-1695. Previous Articles     Next Articles

Reports

ω-苯基-(2S)-N-叔丁氧羰基氨基酸乙酯的制备

丁传勇a,马汝建b,荣国斌*,a   

  1. (a华东理工大学化学与制药学院 上海 200237)
    (b无锡药明康德新药开发有限公司 上海 200131)
  • 收稿日期:2005-01-18 修回日期:2006-05-27 发布日期:2006-11-21
  • 通讯作者: 荣国斌

Preparation of ω-Phenyl-2S-N-Boc-amino Acid Ethyl Ester

DING Chuan-Yonga,MA Ru-Jianb,RONG Guo-Bin*,a   

  1. (a Department of Chemistry and Pharmaceutics, East China University of Science and Technol-ogy, Shanghai 200237)
    (b Wuxi PharmaTech Co., Ltd., Shanghai 200131)
  • Received:2005-01-18 Revised:2006-05-27 Published:2006-11-21
  • Contact: RONG Guo-Bin

N-Boc-pyroglutamic ethyl ester was treated with Grignard reagents to afford ω-phenyl-δ- oxo-2S-N-Boc-amino acid ethyl esters, which were subsequently reduced either with one-pot reaction in the presence of TsNHNH2 and NaBH(OAc)3 or Pd/C catalyzed hydrogenation to yield the desired ω-phenyl-2S-N-Boc-amino acid ethyl esters.

Key words: preparation, N-Boc-pyroglutamic ethyl ester, ω-phenyl-2S-N-Boc-amino acid ethyl ester