Improved stereoselectivity in the heterogeneous catalytic synthesis of enalapril obtained through multidimensional screening

被引：23

作者：

Huffman, MA ^{[1
]}

Reider, PJ ^{[1
]}

机构：

[1] Merck Res Labs, Dept Proc Res, Rahway, NJ 07065 USA

来源：

TETRAHEDRON LETTERS | 1999年 / 40卷 / 05期

关键词：

D O I：

10.1016/S0040-4039(98)02590-8

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A multidimensional screening of catalysts and additives led to the discovery of improved conditions for the diastereoselective reductive amination which produces enalapril. Additives acetic acid and potassium fluoride, which in isolation are detrimental, work together to improve the SSS : RSS selectivity with Ra-Ni in ethanol to 17 : 1 from 11 : 1. (C) 1999 Elsevier Science Ltd. All rights reserved.

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页码：831 / 834

页数：4

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