西地那非类似物的合成  

Synthesis of Sildenafil Analogues

作　　者：帅放文 黄祖云 王向峰 龙泽昕 肖江 

机构地区：[1]湖南省药用辅料工程技术研究中心有限公司,湖南长沙410331 [2]湖南尔康制药股份有限公司,湖南长沙410331

出　　处：《合成化学》2016年第5期454-456,460,共4页Chinese Journal of Synthetic Chemistry

摘　　要：报道了一种合成西地那非类似物的新方法。以邻丙氧基苯甲酸为原料,经5步反应制得西地那非类似物的关键中间体——硫代西地那非氯{1-甲基-3-丙基-5-(2-丙氧基-5-氯磺酰苯基)-1,6-二氢-7H-吡唑并[4,3-d]嘧啶-7-硫酮}(7);7与哌嗪衍生物反应合成了4个新型的西地那非类似物,收率72.3%~80.9%,纯度99.0%,其结构经~1H NMR和ESI-MS表征。A novel route for synthesizing sildenafil analogue was reported. The key intermediate,sulfur-substituted sildenafil chloride（ 7）,was obtained by a five-step reaction from 2-propoxybenzoic acid. Four novel sildenafil analogues（ 9a ~ 9d） were synthesized by the reaction of 7 with piperazine derivatives. The yield and purity of 9a ~ 9d were 72. 3% ~ 80. 9% and 99. 0%,respectively. The structures were characterized by^1 H NMR and ESI-MS.

关 键 词：邻丙氧基苯甲酸 哌嗪 西地那非类似物 中间体合成 药物合成 

分 类 号：O621.3[理学—有机化学] R914.5[理学—化学]