Kilogram scale synthesis of the pyrazinone acetic acid core of an orally efficacious thrombin inhibitor

被引：21

作者：

Fleitz, FJ ^{[1
]}

Lyle, TA

Zheng, N

Armstrong, JD

Volante, RP

机构：

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

[2] Merck Res Labs, Dept Med Chem, W Point, PA 19486 USA

来源：

SYNTHETIC COMMUNICATIONS | 2000年 / 30卷 / 17期

关键词：

D O I：

10.1080/00397910008086927

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A multi-kilogram scale synthesis of the orally efficacious thrombin inhibitor 1 has been achieved via construction of the pyrazinone core from an unsymmetric oxalic diamide. Key features include judicious choice of reagents to minimize side products, a key ruthenium catalyzed oxidation, and development of reaction conditions amenable to large-scale synthesis.

引用

页码：3171 / 3180

页数：10

共 16 条

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