The Combination of Hydroformylation and Biocatalysis for the Large-Scale Synthesis of (S)-Allysine Ethylene Acetal

被引：14

作者：

Cobley, Christopher J. ^{[1
]}

Hanson, Christopher H. ^{[2
]}

Lloyd, Michael C. ^{[1
]}

Simmonds, Shaun ^{[1
]}

机构：

[1] Dr Reddys Labs EU Ltd, Chirotech Technol Ltd, Cambridge CB4 0GH, England

[2] Dr Reddys Labs EU Ltd, Mirfield WF14 8HZ, W Yorkshire, England

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2011年 / 15卷 / 01期

关键词：

ASYMMETRIC HYDROFORMYLATION; LIGANDS;

D O I：

10.1021/op100258j

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The compound, (S)-2-amino-5-[1,3]dioxolan-2-yl-pentanoic acid [(S)-allysine ethylene acetal], is a key intermediate in a number of angiotension-I converting enzyme (ACE) and neutral endopeptidase (NEP) inhibitors currently in clinical trials. Through a combination of our hydroformylation and biocatalysis technologies we have developed an efficient five-step synthetic route to this material starting from crotonaldehyde. The development of this process, leading to a large-scale commercial manufacturing campaign, is described in this paper.

引用

页码：284 / 290

页数：7

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