First scale-up to production scale of a ring closing metathesis reaction forming a 15-membered macrocycle as a precursor of an active pharmaceutical ingredient

被引：142

作者：

Nicola, T ^{[1
]}

Brenner, M ^{[1
]}

Donsbach, K ^{[1
]}

Kreye, P ^{[1
]}

机构：

[1] Boehringer Ingelheim Pharma GmbH & Co KG, Dept Proc Dev, D-55216 Ingelheim, Germany

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2005年 / 9卷 / 04期

关键词：

D O I：

10.1021/op0580015

中图分类号：

O69 [应用化学];

学科分类号：

081704 [应用化学];

摘要：

BILN 2061 ZW (4) is a new chemical entity which shows promising results against the Hepatitis C virus. The major issue in the synthetic route represents the scale-up of a ring closing metathesis reaction to form a 15-membered macrocycle. The parameters chosen for the macrocyclization are discussed, and the experience during large scale synthesis, trouble shooting, and possible improvements for future campaigns are described.

引用

页码：513 / 515

页数：3

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