Practical Synthesis of N-{4-[(2-Methyl-4, 5-dihydroimidazo [4, 5-d][1] benzazepin-6 (1 H)-yl) carbonyl] phenyl} biphenyl-2-carboxamide Monohydrochloride: an …

…, A Yamazaki, H Iwamoto, S Sakamoto

Index: Tsunoda, Takashi; Yamazaki, Atsuki; Iwamoto, Hidenori; Sakamoto, Shuichi Organic Process Research and Development, 2003 , vol. 7, # 6 p. 883 - 887

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Citation Number: 11

Abstract

A novel, reliable, and cost-effective synthetic route to N-{4-[(2-methyl-4, 5-dihydroimidazo [4, 5-d][1] benzazepin-6 (1 H)-yl) carbonyl] phenyl} biphenyl-2-carboxamide monohydrochloride (1, YM087), a potent Arginine vasopressin antagonist, has been developed. Using moisture-controlled potassium carbonate, imidazole formation from α- bromoketone furnished imidazobenzazepine, avoiding potential oxazole-ring formation. ...