Experiment 1 Recrystallization of
Acetanilide1



實驗一乙酰苯胺重結晶7



Experiment 2 Synthesis of Aspirin12



實驗二阿司匹林的合成17



Experiment 3 Synthesis of Paracetamol22



實驗三撲熱息痛的合成27



Experiment 4 Synthesis of Benorilate31



實驗四苯樂來的合成37



Experiment 5 Synthesis of Sulfacetamide Sodium42



實驗五磺胺醋酰鈉的合成49



Experiment 6 Synthesis of Benzocaine55



實驗六苯佐卡因的合成64



Experiment 7 Synthesis of Ciprofloxacin Monohydrochloride Monohydrate71



實驗七鹽酸環丙沙星的合成81



Experiment 8 Synthesis of Phenytoin Sodium89



實驗八苯妥英鈉的合成95



Experiment 9 Synthesis of Neostigmine Bromide100



實驗九溴新斯的明的合成107



Experiment 10 Synthesis of Dyclonine Hydrochloride113



實驗十鹽酸達克羅寧的合成119



Appendix 1 Experimental Report Template124



附錄一實驗報告模板127



Appendix 2 Reference Answer for the Discussion Questions130



附錄二思考題參考答案135



Appendix 3 Common Instruments（常用儀器）140



References（參考文獻）142

為適應我國本科教學國際化的發展趨勢，根據藥物化學實驗課程的基本要求，結合我們多年的教學經驗和科研工作，編寫了這本《藥物化學實驗雙語教程(Experiments of Medicinal Chemistry)》。



本書包括10個化學藥物合成實驗，實驗一至實驗八為我們多年藥物化學實驗教學實踐的總結，實驗九和實驗十為編者科研工作的結果。在化學藥物合成實驗的安排上，本書按照從基礎操作到綜合實驗的順序進行編寫；在內容上，本書不僅給出了實驗原理、操作過程、注意事項和思考題，而且給出了藥物分子和靶標的作用機制圖示、主要原料和中間體的物理常數、實驗裝置、安全提示和思考題參考答案。旨在強調藥物化學理論教學與實驗的關聯，關注學生實驗能力和科研素質培養。10個化學藥物合成實驗的難易程度和實驗學時有明顯的區分度，可滿足不同專業和不同層次學生的教學需求。



本教材的實驗一、實驗二、實驗七、實驗九由李雯、劉宏民編寫，實驗三、實驗四由陳亞靜編寫，實驗五由丁麗娜編寫，實驗六由張恩編寫，實驗八由鄭一超編寫，實驗十由張秋榮編寫，全書由尤啟鼕教授審訂。書中藥物分子和靶標的作用機制部分由丁麗娜及其研究生閻影、馬超亞、王志正、高琦冰、孫旭東和楊晶等借助MOE軟件進行模擬研究編寫而成。留學中國的博士研究生Moges Dessale
Asmamaw、研究生常英傑、李瑞鵬及本科參與了本書的語言潤色工作。藥物化學實驗雙語教材的建設，任重而道遠。



《藥物化學實驗雙語教程(Experiments of Medicinal Chemistry)》采用中英雙語體繫編寫，可作為普通高等醫藥院校藥學類各專業學生（包括留學生）的實驗教材，也可供其他藥學相關專業師生參考使用。







編者



2019年3月















In order to adapt to the development trend of internationalization of
undergraduate teaching in our country, according to the basic requirements of
pharmaceutical chemistry experiment course combined with our years of teaching
experience and scientific research work, this “bilingual
course of pharmaceutical chemistry experiment” has been
compiled.



In this textbook, 10 synthetic experiments of chemical drugs are
included.Experiments 1 through 8 are the summaries of many years teaching
practices, Experiments 9 and 10 are the results of the editors’ scientific research work.They are arranged by the order from basic
to comprehensive gradually.In each experiment, more than the experiment
principle, operation process, notes and discussion questions are given, the
action mechanism diagrams of drug molecule and target, physical constants of
key raw materials and intermediates, experimental equipments, safety tips and
reference answers of discussion questions are described.This textbook
emphasizes the relationship between theoretical teaching and experiment of
pharmaceutical chemistry, and pays attention to the cultivation of students’ experimental ability and scientific research quality.There is a
clear distinction between the difficulty and time of 10 experiments to meet the
teaching needs of students from different majors and levels.



Experiments 1, 2, 7 and 9 of this textbook were written by Wen Li and Hongmin
Liu, Experiments 3 and 4 by Yajing Chen, Experiment 5 by Lina Ding, Experiment
6 by En Zhang, Experiment 8 by Yichao Zheng and Experiment 10 by Qiurong
Zhang.This textbook was revised by Professor Qidong You.The mechanistic studies
between the drug molecule and the corresponding target were investigated and
written by Lina Ding and her graduate students Ying Yan, Chaoya Ma, Zhizheng
Wang, Qibing Gao, Xudong Sun and Jing Yang with the help of MOE software.We
appreciate the foreign PhD student Moges Dessale Asmamaw, graduate students
Yingjie Chang, Ruipeng Li and undergraduate student Linyuan Zhu who involved in
the language correction of this textbook.The construction of bilingual
textbooks is on the developing way.



This textbook is compiled in a Chinese-English bilingual system and can be used
in the experimental teaching of pharmaceutical students (including foreign
students) in medical colleges and universities.







Editors



March 2019