PROCESS FOR PRODUCING BENZODIAZEPINE DERIVATIVES AND SALTS THEREOF

摘要

Title cpds. of formula (I): where R1 = H or CnH2nR5, where n = 1-4 and R5 = H, (2-5C) alkenyl, trihalo (1-4C) alkyl, 1-4C alkoxy, (1-4C) thioalkyl, (1-4C) sulphonylalkyl, aryloxy 2-5C alkenyloxy, (3-6C) cycloalkyl or NR6R7, where R6 and R7 = H, or (1-4C) alkyl or NR6R7 = a 5-6 membered opt. substd. heterocyclic gp. opt. contng. other heteroatoms; R2 = H or (1-4C) alkyl; R3 = (1-4C) alkyl, (3-6C) cycloalkyl, or C6H3HY where X and Y = H, hal (1-4C) alky or CF3; and R4 = H, hal, NO2 or CF3, are prepd. by reducing the corresp 1,3-dihydro-2H-1,4-benzodiazepine-2-ones with a complex metal hydride e.g. LiAlH4 and a Lewis acid e.g. Al2Cl6 in a solvent, e.g. Et2O. I are sedatives, tranquillisers, and muscle relaxants.