The development of a robust process for a CRF1 receptor antagonist

…, Y Tai-Yuen, C Pathirana, JP Sherbine

Index: Broxer, Sevrine; Fitzgerald, Monica A.; Sfouggatakis, Chris; Defreese, Jessica L.; Barlow, Evan; Powers, Gerald L.; Peddicord, Michael; Su, Bao-Ning; Tai-Yuen, Yue; Pathirana, Charles; Sherbine, James P. Organic Process Research and Development, 2011 , vol. 15, # 2 p. 343 - 352

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Citation Number: 8

Abstract

A scalable and robust process was developed for the preparation of pexacerfont (2), a pyrazolotriazine corticotropin-releasing factor receptor 1 antagonist (CRF1). The formation of the core hydroxypyrazolotriazine moiety was achieved through two consecutive cyclizations of a semicarbazide, employing reaction conditions that are significantly milder than those reported in the literature. Further conversion to the key chloropyrazolotriazine intermediate ...