CAS 160129-45-3: 7-CHLORO-1,2,3,4-TETRAHYDRO-BENZO[B]AZEPIN-5-ONE

7-Chloro-1,2,3,4-tetrahydrobenzo[b]azepin-5-one

7-Chloro-1,2,3,4-tetrahydrobenzo[b]azepin-5-one (7CTB) is a synthetic vasopressin analogue that is used as a vasopressin receptor antagonist. It is a competitive inhibitor of the vasopressin V2 receptor and has been shown to be effective in the treatment of diabetes insipidus. 7CTB has also been shown to bind to and inhibit the binding of arginine, an acid binding agent, preventing hydrolysis reactions with other compounds. 7CTB has been shown to be an effective agent for the treatment of congestive heart failure and chronic kidney disease in animal models. The synthesis process involves sulfonylation followed by dieckmann condensation and organic solvent extraction.

Applications 7-Chloro-1,2,3,4-tetrahydrobenzo[b]azepin-5-one is an intermediate in the synthesis of Tolvaptan (T536650) (OPC-41061), an orally active nonpeptide arginine vasopressin V2 receptor antagonist References Kondo, K., et al.: Bioorg. Med. Chem., 7, 1743 (1999);