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苯胺与对甲苯磺酰氯反应得对甲苯磺酰苯胺,与4-氯丁酸甲酯在聚乙二醇400和混合碱(Na OH+Na2CO3)存在下发生N-烷基化反应,然后水解得4-(N-对甲苯磺酰基苯胺基)丁酸,再在多聚磷酸作用下经傅-克酰基化反应后,经氯代反应得4-氯-1-对甲苯磺酰基-1,2,3,4-四氢-5H-苯并氮?-5-酮,再与盐酸乙脒反应制得2-甲基-6-对甲苯磺酰基-1,4,5,6-四氢咪唑并[4,5-d][1]苯并氮?,总收率约54.3%。
Aniline and p-toluenesulfonyl chloride were p-toluenesulfonanilide, methyl 4-chlorobutanoate in the presence of polyethylene glycol 400 and mixed alkali (Na OH + Na2CO3) in the presence of N-alkylation reaction, and then hydrolyzed 4- (N-p-toluenesulfonyl anilino) butanoic acid, and then under the action of polyphosphoric acid by Friedel-Crafts acylation, the reaction of 4-chloro-1-p-toluenesulfonyl-1,2 , 3,4-tetrahydro-5H-benzazepin-5-one, and then reacted with acetamidine hydrochloride to obtain 2-methyl-6-p-toluenesulfonyl-1,4,5,6-tetrahydroimidazole And [4,5-d] [1] benzazepine, the total yield of about 54.3%.