摘要
盐酸多西环素为重要的人兽两用药,其生产过程中的脱氯和不对称氢化反应对产品的收率和质量有重要影响。以11α-氯代甲烯土霉素为起始原料,自制钯炭为催化剂,经脱氯、氢化和转盐3步反应合成了盐酸多西环素,总收率达58.4%,其结构经~1H NMR确证。
Doxycycline hydrochloride is an important antibiotic used for human and animal.Dechlorination and asymmetric hydrogenation were important to the yield and quality in the preparation of doxycycline.Starting from 11α-chloro-metacycline,doxycycline hydrochloride was synthesized through a three-step reaction of dechlorination,hydrogenation,and salification with the overall yield of 58.4%.The structure was confirmed by^1 H NMR.
作者
徐桂清
朱荣荣
毛雪莹
毛龙飞
吴斗灿
高原
姜玉钦
李伟
XU Gui-qing;ZHU Rong-rong;MAO Xue-ying;MAO Long-fei;WU Dou-can;GAO Yuan;JIANG Yu-qin;LI Wei(Key Laboratory of Green Chemical Media and Reactions,Ministry of Education,Collaborative Innovation Centre of Henan Province for Green Manufacturing of Fine Chemicals,Henan Engineering Research Center of Chiral Hydroxyl Pharmaceutical,School of Chemistry and Chemical Engineering,Henan Normal University,Xinxiang 453007,China;Qian Weichang College,Shanghai University,Shanghai 200444,China;Hennan Ziweixing Chemistry Co.,Ltd.,Xinxiang 4453011,China)
出处
《合成化学》
CAS
北大核心
2019年第2期145-148,共4页
Chinese Journal of Synthetic Chemistry
基金
河南省科技创新杰出青年基金资助项目(164100510015)
关键词
盐酸多西环素
脱氯反应
不对称氢化反应
药物合成
.doxycycline hydrochloride
dechlorination
asymmetric hydrogenation
drug synthesis
