摘要 |
1392681 Benzodiazepine derivatives F HOFFMANN-LA ROCHE & CO AG 20 Aug 1973 [21 Aug 1972 14 May 1973] 39218/73 Heading C2C Benzodiazepine derivatives of general formula where R 1 is a hydrogen or halogen atom or a nitro or trifluoromethyl group, R 2 is a hydrogen atom or a C 1 -C 5 alkyl group, and R 3 is a phenyl, o-halophenyl or 2-pyridyl group are prepared by reacting a compound of general formula where X is Cl, Br or I, with hexamethylenetetramine in an inert organic solvent and in the presence of ammonia, with the possible isolation of an intermediate of general formula The ammonia may be formed in situ from an ammonia-generating agent, e.g. ammonium carbonate, and the hexamethylenetetramine may also be formed in situ from formaldehyde and ammonia. |