Synthesis and purification of 6-ethoxy-4-oxo-1,4-dihydro-[1,5]naphthyridine-3-carboxylic acid benzylamide

被引：15

作者：

Beaudin, J ^{[1
]}

Bourassa, DE ^{[1
]}

Bowles, P ^{[1
]}

Castaldi, MJ ^{[1
]}

Clay, R ^{[1
]}

Couturier, MA ^{[1
]}

Karrick, G ^{[1
]}

Makowski, TW ^{[1
]}

McDermott, RE ^{[1
]}

Meltz, CN ^{[1
]}

Meltz, M ^{[1
]}

Phillips, JE ^{[1
]}

Ragan, JA ^{[1
]}

Ripin, DHB ^{[1
]}

Singer, RA ^{[1
]}

Tucker, JL ^{[1
]}

Wei, LL ^{[1
]}

机构：

[1] Pfizer Inc, Pfizer Global Res Div, Chem Res & Dev, Groton, CT 06340 USA

来源：

ORGANIC PROCESS RESEARCH & DEVELOPMENT | 2003年 / 7卷 / 06期

关键词：

D O I：

10.1021/op0341061

中图分类号：

O69 [应用化学];

学科分类号：

081704 [应用化学];

摘要：

The synthesis of 6-ethoxy-4-oxo-1,4-dihydro-[1,5]naphthyridine-3-carboxylic acid benzylamide (1) on multikilogram scale is described. The major challenge for the synthesis of this quinolone GABA partial agonist was in the isolation of product of acceptable purity for clinical studies due to the insolubility of this compound. Also described are efforts to circumvent a high-temperature cyclization required for the synthesis of the quinolone ring system.

引用

页码：873 / 878

页数：6

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