The stability of 1-cyclopropylmethyl-5(o-fluorophenyl)-7-chloro-1,3-dihydro-2H-1,4-benzodiazepin-2-one (KB-509) in aqueous solution

Autor: Sugimoto Isao, Awata Norio, Akimoto Koichi, Fujiwara Shigeru
Rok vydání: 1979
Předmět:
Zdroj: International Journal of Pharmaceutics. 3:109-115
ISSN: 0378-5173
DOI: 10.1016/0378-5173(79)90072-3
Popis: The main degradation of 1-cyclopropylmethyl-5-(o-fluorophenyl)-7-chloro-l,3-dihydro-2H-1,4-benzodiazepin-2-one (KB-509) in aqueous solution involves a two-step consecutive mechanism. The first step is the hydrolysis of KB-509, yielding 5-chloro-cyclopropyl-methylamino-2'-fluorobenzophenone (1) and glycine. The second step is the ring closure of the benzophenone derivative to give 2-chloro-10-cyclopropylmethyl-9-acridanone (2) at all pH regions.
Databáze: OpenAIRE