Large-scale candoxatril asymmetric hydrogenation

被引：23

作者：

Bulliard, M ^{[1
]}

Laboue, B ^{[1
]}

Lastennet, J ^{[1
]}

Roussiasse, S ^{[1
]}

机构：

[1] PPG SIPSY, ZI Croix Cadeau, F-49242 Avrille, France

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2001年 / 5卷 / 04期

关键词：

D O I：

10.1021/op010005w

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

Ruthenium-catalyzed asymmetric hydrogenation was used to prepare tons of a key chiral succinate intermediate for clinical trials quantities of candoxatril. MeOBiphep was used as the ligand, and the catalyst was generated in situ from RuCOD-Bismethylallyl. THF was the best cosolvent for the reaction leading to a selective hydrogenation and a process which was readily amenable on large scale.

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页码：438 / 441

页数：4

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