A method for the production of 1 - hydroxyalkyl - 5 - (o - halophenyl) - 1,3 - dihydropyridines - 2h - 1,4 - benzodiazepine - 2 - on - derivatives

摘要

1-Hydroxyalkyl-benzodiazepinones (I) and acid salts - (R1 = H or halogen, 1-4C alkoxy, NO2, CF3 or CN; R2 = H, 1-4C alkyl, aralkyl or Ph; R3 = pyridyl or R4, R5 being (same or diff.) H, halogen, 1-4C alkyl, CF3 or CN; n = 1-4), for use as tranquillisers, muscle relaxants, spasmolytics, anticonvulsants and hypnotics, are obtained in high yields and are easily purified. 2-Hydroxyalkylamino-benzophe nones are condensed with oxazolidiones in organic solvents in presence of acid at 0-30 degrees. In an exmaple, 1-(beta-hydroxyethyl)-5-phen yl-7-chloro-1,3-dihyro-2H-1,4-benzodi- azepin-2-one is obtained (m.pt. 158-160 degrees) from 1 g. 2-(beta-hydroxyethyl)-amino-5-chloro-benzo phenone and 1.2g. oxazoli-2,5-dione in CH2cL2in presence of HCl.