(4-羟基-3-甲氧基苯基)(2-甲基哌啶-1-基)甲酮的合成  

Synthesis of(4-hydroxy-3-methoxyphenyl)(2-methylpiperidin-1-yl)methanone

作　　者：于芳蕾 吉彦彬 徐小娜 张娟[1] YU Fang-lei;JI Yan-bin;XU Xiao-na;ZHANG Juan(School of pharmaceutical&Chemical Engineering,Xianyang Vocational Technical College,Xianyang 712000,China;Xi'an Gas Heating Service Center,Xi'an 710000,China)

机构地区：[1]咸阳职业技术学院医药化工学院,陕西咸阳712000 [2]西安市燃气供热服务中心,陕西西安710000

出　　处：《化学工程师》2023年第6期9-13,共5页Chemical Engineer

基　　金：咸阳职业技术学院博士科研基金项目(2021BK01);咸阳职业技术学院横向基金项目(No.H2022-22)。

摘　　要：本文报道了(4-羟基-3-甲氧基苯基)(2-甲基哌啶-1-基)甲酮(1a)的合成。以4-羟基-3-甲氧基苯甲酸(2)和2-甲基哌啶(3)为原料,经缩合反应得到目标化合物(1a)。并考察该反应工艺,确定适宜的反应条件为:物料比为n(3)∶n(2)=1.8∶1、反应溶剂为N,N-二甲基甲酰胺、反应温度为40℃、反应时间为2h。在该条件下,产物(1a)收率达到88.6%。对该反应工艺的拓展应用发现,该条件同样适用于4-羟基-N,3-二甲氧基-N-甲基苯甲酰胺(1b)的合成,收率达到90.3%。产物结构经过^(1)H NMR和^(13)C NMR表征确证。The synthesis of(4-hydroxy-3-methoxyphenyl)(2-methylpiperidin-1-yl)methanone(1a)was reported.The target compound(1a)was synthesized from 4-hydroxy-3-methoxybenzoic acid(2)and 2-methylpiperidine(3)by condensation reaction.The reaction conditions were investigated,and the suitable conditions for the condensation reaction were determined as follows:material ratio of n(3)∶n(2)=1.8∶1,solvent is N,N-dimethylformamide,the reaction temperature is 40℃and reaction time is 2h.Under these conditions,the yield of product(1a)was up to 88.6%.It was found that this condition was also suitable for the synthesis of 4-hydroxy-N,3-dimethoxy-N-methylbenzamide(1b)in a yield of 90.3%.The structure of the products were characterized by ^(1)H NMR and ^(13)C NMR.

关 键 词：哌啶衍生物 Weinreb酰胺 缩合反应 合成 

分 类 号：TQ463[化学工程—制药化工]