Second-Generation Process for the HCV Protease Inhibitor BILN 2061: A Greener Approach to Ru-Catalyzed Ring-Closing Metathesis

被引：79

作者：

Farina, Vittorio ^{[1
]}

Shu, Chutian ^{[1
]}

Zeng, Xinazhong ^{[1
]}

Wei, Xudong ^{[1
]}

Han, Zhengxu ^{[1
]}

Yee, Nathan K. ^{[1
]}

Senanayake, Chris H. ^{[1
]}

机构：

[1] Boehringer Ingelheim Pharmaceut Inc, Dept Chem Dev, Ridgefield, CT USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2009年 / 13卷 / 02期

关键词：

RUTHENIUM CARBENES; OLEFIN METATHESIS; MACROCYCLIZATION; BILN-2061; SCALE; RCM;

D O I：

10.1021/op800225f

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The ring-closing metathesis (RCM) step, a key reaction in our process to BILN 2061, was dramatically improved from the first-generation process by the selection of a more appropriate substrate as well as the use of a more effective catalyst. The two RCM reactions are compared in detail using criteria that are of high significance to the process chemist.

引用

页码：250 / 254

页数：5

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