Akimoto Koichi, F. Shigeru, Awata Norio
Aug 1, 1979
Citations
0
Influential Citations
2
Citations
Journal
International Journal of Pharmaceutics
Abstract
Abstract 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.