| 摘要 |
Compounds of the general formula <FORM:1067745/C2/1> (in which each of X and Y represents hydrogen, chlorine, bromine, nitro, halo-(C1- 6 alkyl) or C1- 6 alkylsulphonyl, R is hydrogen or C1- 6 alkyl and Ar is phenyl optionally substituted by chlorine, bromine, halo-(C1- 6 alkyl), C1- 6 alkoxy or C1- 6 alkyl) and their N-oxides and 3-acyloxy derivatives are prepared by oxidizing the corresponding 5 - aryl - 1,3,4,5 - tetrahydro-2H-1,4 - benzodiazepin - 2 - one, optionally followed by conversion to the N-oxide (if not obtained directly) or 3-acyloxy derivative (by reaction with hydrogen peroxide or peracetic acid in an oxidation-resistant solvent in the presence of an acylating agent); the 3-acyloxy derivatives may alternatively be prepared directly by reacting the starting material with hydrogen peroxide or peracetic acid in an oxidation-resistant solvent in the presence of an acylating agent. The starting materials may be prepared by cyclizing a corresponding compound of the general formula <FORM:1067745/C2/2> (in which M is hydrogen or an alkyl radical). The preparation of N-(2-amino-5-chloro-a -phenylbenzyl) glycine, its ethyl ester and the dihydrochloride of the latter and 7-chloro-5-phenyl - 1,3,4,5 - tetrahydro - 2H - 1,4 - benzodiazepin-2-one hydrochloride is described. |
