Development of a Chemoenzymatic Route to (R)-Allyl-(3-amino-2-(2-methylbenzyl)propyl)carbamate

被引：9

作者：

Lindhagen, Marika ^{[1
]}

Klingstedt, Tomas ^{[1
]}

Andersen, Soren M. ^{[1
]}

Mulholland, Keith R. ^{[2
]}

Tinkler, Laura ^{[3
]}

McPheators, Gary ^{[3
]}

Chubb, Richard ^{[3
]}

机构：

[1] AstraZeneca R&D, S-43183 Molndal, Sweden

[2] AstraZeneca Pharmaceut Dev, Macclesfield SK10 2NA, Cheshire, England

[3] Onyx Sci Ltd, Sunderland SR5 2TQ, England

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2016年 / 20卷 / 01期

关键词：

DESYMMETRIZATION; DERIVATIVES;

D O I：

10.1021/acs.oprd.5b00326

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

A chemoenzymatic route to (R)-allyl-(3-amino-2-(2-methylbenzyl)propyl)carbamate (1-(R)) has been developed on a kilogram scale. The key intermediate, 2-(2-methylbenzyl)propane-1,3-diamine 4, was isolated as a tartrate salt in a three-step sequence starting from 2-methylbenzyl chloride. The subsequent lipase-catalyzed desymmetrization was optimized, and 1-(R) was isolated as the d-tartrate salt.

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收藏

页码：65 / 69

页数：5

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