发明名称 Procédé de production de nouveaux dérivés de la benzimidazolinone et de leurs sels d'addition avec les acides
摘要 New compounds of formula <FORM:1046311/C2/1> where Ar is phenyl, halophenyl, lower (i.e. 1-5 C) alkylphenyl or lower alkoxyphenyl, R is hydrogen, lower alkyl, lower alkylcarbonyl, benzoyl, hydroxymethyl, halomethyl, lower alkoxymethyl, cyanomethyl or cyano- CH(R2)CH(R2)-, R2 being hydrogen or methyl, R1 is hydrogen or methyl, and n is 1 or 2, and non-toxic acid addition salts thereof, are prepared by methods comprising (1) reaction of an Ar-alkenyl-chloro or -bromo compound with a 4-substituted-piperidine, (2) introduction of a hydroxymethyl group R with formaldehyde, from which halomethyl compounds are obtained and thence alkoxymethyl or cyanomethyl compounds, (3) introduction of alkyl groups R, (4) introduction of alkylcarbonyl or benzoyl groups R, (5) introduction of cyano- CH(R2)CH(R2)- groups R using a ,b -unsaturated nitriles. Starting materials prepared are: 1-(4-fluorophenyl) - 4 - chloro - 1 - butene, 2 - phenyl - 5 - bromo - 2 - pentene, 2 - (4 - fluorophenyl) - 5 - bromo - 2 - pentene, 2 - (4 - methoxyphenyl) - 5 - chloro - 2 - pentene, 2 - (4 - chlorophenyl) - 5 - chloro - 2 - pentene and 2 - (4 - methylphenyl) - 5-chloro-2-pentene, all obtained from corresponding phenyl - cyclopropyl - carbinols with halogenating agents; dl - cyclopropyl - 4- (methoxy-, chloro-, methyl-)phenyl - methyl-carbinols are prepared from ketones and Grignard reagents.
申请公布号 FR1455875(A) 申请公布日期 1966.10.21
申请号 FR19650015918 申请日期 1965.05.05
申请人 JANSSEN PHARMACEUTICA, NAAMLOZE VENNOOTSCHAP 发明人
分类号 C07C33/34;C07C33/50 主分类号 C07C33/34
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