摘要:本文设计了一条合成α,α-二苯基-4-哌啶甲醇的新路线。采用以4-哌啶甲酸为原料,经N-酰基化反应,傅克酰基化反应等合成α,α-二苯基-4-哌啶甲醇。在N-酰基化反应中经过选择比较最终选定乙酸酐为酰基化试剂,酰氯化反应中选择氯化亚砜为酰氯化试剂,同时对各步反应中的反应温度、反应时间、原料投料比、催化剂用量等工艺参数进行筛选和优化,确定了最佳反应条件。该工艺操作简便,节约成本,可行性高,适合于工业化生产。4975
关键词:4-哌啶甲酸;N-酰基化反应;傅克酰基化反应;抗组胺类药物
New progress of α,α-diphenyl-4-piperidinomethanol
Abstract:In this paper, we designed the new route for the synthesis of α,α-diphenyl-4-piperidinomethanol . The new project uses the 4- piperidine formic acid as raw material to synthesize α,α-diphenyl-4-piperidinomethanol, which was passed by N-acylation, Friedel-Crafts acylation, and other reactions .In the preparation of N-acylation step, the acetic anhydride was chose as Acylation reagents and in the preparation ofFriedel-Crafts acylation ,the sulfoxide chloride was chose as Acylation reagents. At the same time , The reaction temperature, reaction time, dosage of catalyst, raw material ratio for each reaction step is selected and optimized. The process is simple, cost saving, high feasibility, and suitable for industrialized production。
Keywords:4- piperidine formic acid;N-acylation ;Friedel-Crafts acylation ;
Antihistamine drugs.
目录
1.绪论•1
1.1非索非那定简介1
1.1.1药理特性•2
1.1.2市场前景•4
1.2 α,α-二苯基-4-哌啶甲醇简介5
1.2.1化合物性质•5
1.2.2合成方法•6
1.3 实验方案论证•8
1.4 课题研究内容10
2.实验部分11
2.1 实验试剂和仪器•11
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