阿伐那非的合成工艺研究  

Study on Synthesis of Avanafil

作　　者：梅玫 曹棋 程凤 毛婕 阳静丽 胡华南 Mei Mei;Cao Qi;Cheng Feng;Mao Jie;Yang Jingli;Hu Huanan(Jiujiang Ecological Environment Bureau,Jiangxi,332001;College of Chemistry and Chemical Engineering,Jiujiang University,Jiangxi,332005)

机构地区：[1]九江市生态环境局,江西332001 [2]九江学院化学化工学院,江西332005

出　　处：《当代化工研究》2022年第19期149-151,共3页Modern Chemical Research

基　　金：九江市生态环境局委托项目“九江市有机硅产业发展过程中存在的生态环境问题及对策”(项目编号:8999338)。

摘　　要：以4-氯-2-甲硫基嘧啶-5-羧酸乙酯(2)与3-氯-4-甲氧基苄胺(3)为起始原料,经过亲核取代反应、氧化反应、亲核加成,最后水解后与2-氨甲基嘧啶盐酸盐(9)缩合得到目标产物阿伐那非(1)。反应总收率达74.4%,产品经HPLC检测纯度达99.6%以上,目标产物结构经MS、IR、^(1)H-NMR和^(13)C-NMR确证,部分中间体的化学结构经过MS和^(1)H-NMR确证。Using ethyl 4-chloro-2-methylthiopyrimidine-5-carboxylate(2)and 3-chloro-4-methoxybenzylamine(3)as starting materials,through nucleophilic substitution reaction,oxidation reaction and nucleophilic addition,finally,After hydrolysis,it condenses with 2-pyrimidine ethylamine(9)to obtain the target product avanafi(1).The total yield was74.4%,the purity of the product was more than 99.6%by HPLC,the struc-ture of the target product was confirmed by MS,IR,^(1)H-NMR and ^(13)C-NMR,and the chemical structure of some intermediates was confirmed by MS and ^(1)H-NMR.

关 键 词：阿伐那非 PDE5抑制剂 合成 

分 类 号：TQ423.2[化学工程]