A practical synthesis of a COX-2-specific inhibitor.
作者信息
Davies I W, Marcoux J F, Corley E G, Journet M, Cai D W, Palucki M, Wu J, Larsen R D, Rossen K, Pye P J, DiMichele L, Dormer P, Reider P J
机构信息
Department of Process Research, Merck & Co., Inc., P.O. Box 2000, Rahway, New Jersey 07065, USA.
出版信息
J Org Chem. 2000 Dec 15;65(25):8415-20. doi: 10.1021/jo000870z.
PMID:11112557
Abstract
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.
摘要
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