Process for producing 2-substituted 1,4-benzodiazepine...

Details Process for producing 2-substituted 1,4-benzodiazepine... Process for producing 2-substituted 1,4-benzodiazepine...

C - Chemistry, Metallurgy

07

D

260/240.1

C07D 243/16 (2006.01) C07D 245/06 (2006.01)

Patent

CA 1063107

ABSTRACT OF THE DISCLOSURE 2-substituted 1-methyl-5-phenyl-1,4-benzodiazepines corresponding to the formula Image in which R1 represents a hydrogen or halogen atom, R2 repre- sents a hydrogen atom, a halogen atom or a trifluoromethyl group and R3 represents a hydrogen atom or a C1-6 alkyl group, having pharmacological properties, are prepared by direct alkoxylation or hydroxylation of the mixture of the corres- ponding 2-chloromethyl-1,4-benzodiazepine and 3-chloro-1,5- benzodiazocine as prepared in turn by cyclising a correspond- ing N1-phenyl-N1-methyl-N2-benzoyl-2-hydroxy-1,3-diaminopropane by reaction with an excess of phosphorus oxychloride generally at the boiling point of such phosphorus oxychloride. Several of the 7-bromo-1,4-benzodiazepines so obtained are novel compounds exhibiting extremely valuable and surprising pharmacological properties.

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