A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan

Alejandro Cordero-Vargas (1) , Béatrice Quiclet-Sire (1) , Samir Z. Zard (1)

1 DCSO - Laboratoire de synthèse organique

A practical preparation of benzazepine derivatives using a series of radical and ionic reactions is reported. This approach was applied to the synthesis of tolvaptan, a very promising vasopressin V2 receptor antagonist currently in clinical trials. © 2006 Elsevier Ltd. All rights reserved.

Domains: Chemical Sciences; Organic chemistry

Alejandro Cordero-Vargas, Béatrice Quiclet-Sire, Samir Z. Zard. A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan. Bioorganic and Medicinal Chemistry, 2006, 14 (18), pp.6165-6173. ⟨10.1016/j.bmc.2006.05.070⟩. ⟨hal-00951294⟩