A Scalable Process for the Synthesis of 2-Methyl-1, 4, 5, 6-tetrahydroimidazo [4, 5-d][1] benzazepine Monohydrate and 4-[(Biphenyl-2-ylcarbonyl) amino] benzoic Acid: …

…, A Yamazaki, T Mase, S Sakamoto

Index: Tsunoda, Takashi; Yamazaki, Atsuki; Mase, Toshiyasu; Sakamoto, Shuichi Organic Process Research and Development, 2005 , vol. 9, # 5 p. 593 - 598

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Citation Number: 13

Abstract

A process for the multikilogram synthesis of the dual vasopressin-receptor antagonist, conivaptan hydrochloride, has been developed. This method relies on the introduction of operationally simple chemistry during the final stages of the process when two key intermediates, isolated by crystallization, are reacted to assemble the final molecule. A three- stage sequence has been developed for the synthesis of the first key amine hydrate ...