实验二扑炎痛Benorylate的合成.DOCVIP

Experiment of Medicinal Chemistry 主编：木合布力 编者：郭炬亮、丁海燕、王艳 Department of Medicinal and Organic Chemistry, College of Pharmacy, Xinjiang Medical University September, 2010 Table of Content Experiment 1. Preparation of Aspirin…………………………………………… 1 Experiment 2. Preparation of Paracetamol………………………………….……7 Experiment 3. Preparation of Benorilate…………………………………………11 Experiment 4. Preparation of Chlorobutanolum…………………………………16 Experiment 5. Preparation of Nikethamide………………………………………18 Experiment 6. Stability Study of Procaine Hydrochloride……………………… 22 Experiment 7. Preparation of Biphenyl ketobutyric acd..……………………… 26 Experiment 8. Simple Distillation ………………………………………………31 Experiment 9. Melting point Determination…………………………………… 33 Experiment 10. Recristallization…………………………………………………37 Writing method for laboratory report of Medicinal Chemistry………………….40 附录： 实验一、阿司匹林（Aspirin）的制备………………………………………42 实验二、扑热息痛（Paracetamol）的制备…………………………………45 实验三、苯乐来（Benorilate）的制备………………………………………47 实验四、三氯叔丁醇（Chlorobutanolum）的制备…………………………50 实验五、尼克刹米（Nikethamide）的制备…………………………………51 实验六 盐酸普鲁卡因(Procaine Hydrochloride)的稳定性…………………53 实验七 联苯丁酮酸（Biphenyl ketobutyric acd）的制备…………………55 实验八 简单蒸馏(Simple Distillation)………………………………………57 实验九 熔点测定(Melting point Determination)……………………………59 实验十 重结晶(Recristallization)…….………………………………………61 实验报告格式………………………………………………………………… 64 Annex: Apparatus —— glass equipments and assemblies…………………….65 Experiment 1 Preparation of Aspirin (阿司匹林的制备) Introduction Nearly 19th century, medicinal chemists have isolated the active principle salicylic acid from the willow bark tree, and defined its chemical structure. Since, salicylic acid is widely used as anti-rheumatic and antipyretic analgesic drug in the therapeutic treatment. However, during the long clinical practice, some side effects have been observed for this molecule, as stomach stimulating effects, which can induce uncomfortable symptom and peptic ulcer, etc. Medicinal chemists estimate that the strong stimulating effects of the ph