Method of producing 2-halomethyl-1,4-benzodiazepines

Details Method of producing 2-halomethyl-1,4-benzodiazepines Method of producing 2-halomethyl-1,4-benzodiazepines

C - Chemistry, Metallurgy

07

D

260/240.1

C07D 243/16 (2006.01)

Patent

CA 1088528

ABSTRACT OF THE DISCLOSURE 1-alkyl-2-halomethyl-1,4-benzodiazepines corresponding to the formula Image in which R1 represents a C1-4 alkyl group, R2 represents a hydrogen atom, a halogen atom or a trifluoromethyl group, R3 represents a hydrogen or halogen atom and X represents a chlor- ine or bromine atom, having pharmacological properties, are pre- pared with improved yield by halogenating the corresponding N1- benzoyl-N2-alkyl-N2-phenyl-2-hydroxy-1,3-diaminopropane into the corresponding imidoyl halide and then cyclising that imidoyl halide using a Lewis acid catalyst. The halogenation reaction can be effected directly using phosphorus pentachloride or pen- tabromide or the 2-hydroxy group of the acyldiaminopropane can first be halogenated using phosphorus oxychloride, oxybromide, trichloride or tribromide or thionyl chloride to give the cor- responding 2-haloacyldiamine and the acyl group then halogenated using phosphorus pentachloride or pentabromide to give the imi- doyl halide so permitting intermediate purification of the haloacyldiamine.

237301

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