A flexible approach for the preparation of substituted benzazepines: application to the synthesis of tolvaptan.
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.
Cordero-Vargas
Alejandro
A
Laboratoire de Synthèse Organique associé au CNRS, Ecole Polytechnique, 91128 Palaiseau, France.
Quiclet-Sire
Béatrice
B
Zard
Samir Z
SZ
D001552:Benzazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D015394:Molecular Structure; D013237:Stereoisomerism; D000077602:Tolvaptan
D001552:Benzazepines; D000077602:Tolvaptan