A convenient synthesis of activated enantiomerically pure 2-ethynylaziridines

被引:28
作者
Ohno, H [1 ]
Toda, A [1 ]
Fujii, N [1 ]
Ibuka, T [1 ]
机构
[1] Kyoto Univ, Grad Sch Pharmaceut Sci, Sakyo Ku, Kyoto 6068501, Japan
关键词
D O I
10.1016/S0957-4166(98)00406-6
中图分类号
O61 [无机化学];
学科分类号
070301 ; 081704 ;
摘要
2,3-cis- and 2,3-trans-N-Arylsulfonyl-2-ethynylaziridines with high enantiomeric purity have been synthesized. N-Protected amino aldehydes synthesized from natural alpha-amino acids were successively treated with Ph3P=C(Br)CO2Me, DIBAL, MsCl-Et3N, NaH in DMSO, and tert-BuOK in THF to yield 2-ethynylaziridines in good to high yields. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:3929 / 3933
页数:5
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