1-(4-Fluorophenyl methyl) N-(1-(2-(4-methoxyphenyl)ethyl) 4-piperidinyl) 2-amino benzimidazole is made by (a) cyclising 2-amino (N-4-fluorophenyl methyl) aniline with urea in organic solvent, e.g. triglyme, at 110-220 deg. C; (b) treatment of the prod. with phosphoryl chloride and hydrochloric acid under reflux; (c) reaction with 4-amino piperidine 1-carboxylic acid ethyl ester; and (d) condensn. of the 1-(4-fluorobenzyl) 2-(4-piperidinylamino) benzimidazole formed with p-methoxyphenyl ethyl methyl sulphonate in hot dimethyl formamide in presence of Na2CO3 and KI.
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机译:1-(4-氟苯基甲基)N-(1-(2-(4-甲氧基苯基)乙基)4-哌啶基)2-氨基苯并咪唑是通过(a)使2-氨基(N-4-氟苯基甲基)苯胺环化而制得用尿素在有机溶剂中,例如三甘醇二甲醚,在110-220度C; (b)产品的处理。用磷酰氯和盐酸回流。 (c)与4-氨基哌啶1-羧酸乙酯反应; (d)凝结。 Na 2 CO 3和KI存在下,在热二甲基甲酰胺中与对甲氧基苯基乙基甲基磺酸盐形成的1-(4-氟苄基)2-(4-哌啶基氨基)苯并咪唑的混合物。
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