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
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
收藏
页码:101 / 108
页数:8
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