A practical synthesis of a COX-2-specific inhibitor

被引：76

作者：

Davies, IW ^{[1
]}

Marcoux, JF ^{[1
]}

Corley, EG ^{[1
]}

Journet, M ^{[1
]}

Cai, DW ^{[1
]}

Palucki, M ^{[1
]}

Wu, J ^{[1
]}

Larsen, RD ^{[1
]}

Rossen, K ^{[1
]}

Pye, PJ ^{[1
]}

DiMichele, L ^{[1
]}

Dormer, P ^{[1
]}

Reider, PJ ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Proc Res, Rahway, NJ 07065 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2000年 / 65卷 / 25期

关键词：

D O I：

10.1021/jo000870z

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A number of synthetic strategies to the Cox-2 specific inhibitor 1 have been described. These studies have led to the identification of a novel pyridine construction using annulation of ketone 2 using a vinamidinium species 29 and ammonia in 97% assay yield. Three approaches to the synthesis of ketone 2 are described that allow for its preparation in large quantities in >65% overall yield from methyl 6-methylnicotinate.

引用

收藏

页码：8415 / 8420

页数：6

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