ASYMMETRIC-SYNTHESIS OF BETA-AMINO ACID-DERIVATIVES BY MICHAEL ADDITION TO CHIRAL 2-AMINOMETHYLACRYLATES

被引:26
作者
BARNISH, IT [1 ]
CORLESS, M [1 ]
DUNN, PJ [1 ]
ELLIS, D [1 ]
FINN, PW [1 ]
HARDSTONE, JD [1 ]
JAMES, K [1 ]
机构
[1] PFIZER LTD,SANDWICH CT13 9NJ,KENT,ENGLAND
关键词
D O I
10.1016/S0040-4039(00)91786-6
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
The addition of lithium enolates to chiral aminomethylacrylates 7 and 8 proceeded with excellent diastereodifferentiation (up to 98% de) and provided an expeditious synthesis of homochiral beta-aminomethylglutarates 9 and 10, on a scale of up to 500g. The acrylates 7 and 8, and their antipodes, should be useful synthons for the synthesis of beta-amino acid derivatives.
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页码:1323 / 1326
页数:4
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