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Paper | Regular issue | Vol 63, No. 7, 2004, pp.1555-1561
Published online, 14th May, 2004
DOI: 10.3987/COM-04-10071
Facile Methods for Preparation Thiazolopyridine and Tetrahydrothiazolopyridine Derivatives

Noriyasu Haginoya,* Satoshi Komoriya, Ken Osanai, Toshiharu Yoshino, Tsutomu Nagata, Masatoshi Nagamochi, Ryo Muto, Mitsuhiro Yamaguchi, Takayasu Nagahara, and Hideyuki Kanno

*Medicinal Chemistry Research Laboratory, Daiichi Pharmaceutical Co., Ltd., 16-13, Kitakasai 1-chome, Edsogawa-ku, Tokyo 134, Japan


The improved routes to prepare tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid lithium salts (2 and 3) were developed. Route A is consisted of the improved preparation of thiazolopyridine intermediates, and Route B is applicable for a large scale synthesis of tetrahydrothiazolo[5,4-c]pyridine-2-carboxylic acid derivatives. The methods we developed may serve as facile means for preparing thiazolopyridine and tetrahydrothiazolopyridine derivatives.