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Short Paper | Regular issue | Vol 85, No. 7, 2012, pp.1711-1720
Published online, 18th May, 2012
DOI: 10.3987/COM-12-12481
■ A Facile Synthesis of 5,6-Dihydro-4H-pyrrolo[3,4-d]thiazole and Other Pyrrolidine-Fused Aromatic Ring Systems via One-Step Cyclization from Diols

Kenji Yoshikawa,* Tsutomu Nagata, Toshiharu Yoshino, Yumi Nakamoto, Noriyasu Haginoya, Ryo Muto, Akiyoshi Mochizuki, Hideyuki Kanno, and Toshiharu Ohta

*R & D Division, Daiichi Sankyo Co., Ltd., 1-2-58 Hiromachi, Shinagawa-ku, Tokyo 140-8710, Japan

Abstract

A facile synthetic method of 5,6-dihydro-4H-pyrrolo[3,4-d]thiazole, which is a subunit of a potent factor Xa (fXa) inhibitor was developed. This new approach employs one-step cyclization from a diol and can be applied to the syntheses of other pyrrolidine-fused aromatic ring sytems.