Aminocarbonylation route to tolvaptan

…, T Furuta, T Nishi, S Aki, J Minamikawa

Index: Torisawa, Yasuhiro; Furuta, Takuya; Nishi, Takao; Aki, Shinji; Minamikawa, Jun-ichi Bioorganic and Medicinal Chemistry Letters, 2007 , vol. 17, # 23 p. 6455 - 6458

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Citation Number: 7

Abstract

Tolvaptan is in clinical trial as an orally active vasopressin (V 2 ) antagonist, 1 possessing the key benzazepinone amide structural unit, like other congeners of interest. 2 Under these circumstances, construction of the key amide structural units [ArNH–COAr′] by non-conventional method has become major concern in our research process. We would like to describe herein a synthesis of the tolvapatan intermediate 1 (Scheme 1) utilizing Pd-catalyzed ...