Kilogram-Scale Synthesis of an Inhaled Corticosteroid

被引：5

作者：

Knight, Craig J. ^{[1
]}

Millan, David S. ^{[2
]}

Moses, Ian B. ^{[1
]}

Robin, Aurelie A. ^{[1
]}

Selby, Matthew D. ^{[2
]}

机构：

[1] Pfizer Global Res & Dev, Res API, Sandwich CT13 9NJ, Kent, England

[2] Pfizer Global Res & Dev, Worldwide Med Chem, Sandwich CT13 9NJ, Kent, England

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2012年 / 16卷 / 04期

关键词：

Drug products;

D O I：

10.1021/op200257g

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The development and implementation of a safe and scalable process for the manufacture of corticosteroid PF-4714224 (1) is described. Initial routes used to synthesise analogues from this series directly from fluocinolone acetonide (2) were unsuitable for large-scale use. Key aspects of the route are the efficient and simple method for the preparation of the steroid tetraol (6), acetal formation by reaction of the tetraol with a bisulphite adduct (12), and isolation of the product by sequential recrystallisations.

引用

页码：697 / 703

页数：7

共 11 条

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