Document Type and Number:
Japanese Patent JPS6218554
Kind Code:
B2
Abstract:
1-alkyl-2-halomethyl-1,4-benzodiazepines corresponding to the formula 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 chlorine or bromine atom, having pharmacological properties, are prepared with improved yield by halogenating the corresponding N1benzoyl-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 pentabromide 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 corresponding 2-haloacyldiamine and the acyl group then halogenated using phosphorus pentachloride or pentabromide to give the imidoyl halide so permitting intermediate purification of the haloacyldiamine.
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Inventors:
HORUSUTO TSUOIGUNERU
UORUFUGANGU MIRUKOFUSUKII
HANSU RIIPUMAN
JIIKUFURIITO FUNKE
UERUNERU SHUTOYUUMERU
RORUFU HYUTSUSHENSU
UORUFUGANGU MIRUKOFUSUKII
HANSU RIIPUMAN
JIIKUFURIITO FUNKE
UERUNERU SHUTOYUUMERU
RORUFU HYUTSUSHENSU
Application Number:
JP12235975A
Publication Date:
April 23, 1987
Filing Date:
October 09, 1975
Export Citation:
Assignee:
KALI CHEMIE PHARMA GMBH
International Classes:
C07C67/00; C07C241/00; C07C257/02; C07D243/16; C07D243/28