A practical synthesis of the PDE4 inhibitor, SB-207499, from a cyclohexanone precursor

被引：8

作者：

Badham, NF

Chen, JH

Cummings, PG

Dell'Orco, PC

Diederich, AM

Eldridge, AM

Mendelson, WL

Mills, RJ

Novack, VJ

Olsen, MA

Rustum, AM

Webb, KS

Yang, S

机构：

[1] GlaxoSmithKline Pharmaceut, Dept Synthet Chem, King Of Prussia, PA 19406 USA

[2] Dept Analyt Sci, King Of Prussia, PA 19406 USA

[3] Dept Environm Res, King Of Prussia, PA 19406 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2003年 / 7卷 / 01期

关键词：

D O I：

10.1021/op025584z

中图分类号：

O69 [应用化学];

学科分类号：

081704 ;

摘要：

The synthesis of SB-207499 is described. Investigation and development of new strategies for the homologation of ketone, 4-cyano-4-[3-(cyclopentyloxy)-4-(methoxyphenyl)]-cyclohexan-1-one 2 are described which produce SB-207499. Our ultimate route of synthesis to SB-207499 is robust and operationally simple and produces the final drug substance in good yield and purity.

引用

页码：101 / 108

页数：8