Vardenafil hydrochloride hydrate, BAY-38-9456, Vivanza, Levitra
瓦地那非盐酸盐 伐地那非 伐地那非Chemical Name: 2-[2-Ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)phenyl]-5-methyl-7-propylimidazo[5,1-f][1,2,4]triazin-4(3H)-one hydrochloride trihydrate
CAS No. 224785-91-5 (anhydrous), 224789-15-5 (diHCl), 224785-90-4 (free base, anhydrous)
项目整合开发状态: Launched-2003
项目研究机构: Bayer (Originator), GlaxoSmithKline (Comarketer), Schering-Plough (Comarketer)
合成路线:Cyclization of 2-ethoxybenzamidine (I) with 2-butyramidopropionic acid (II) and ethoxalyl chloride (III) by means of DMAP in refluxing pyridine gives 2-(2-ethoxyphenyl)-5-methyl-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-4-one (IV),which is sulfonated with chlorosulfonic acid to provide the sulfonyl chloride (V).Finally,this compound is condensed with 1-ethylpiperazine (VI) in dichloromethane.
📌 参考资料/链接：
参考文献标题:2-Phenyl substd.imidazotriazinones as phosphodiesterase inhibitors
文献作者:Perzborn,E.; Keldenich,J.; Schlemmer,K.-H.; Haning,H.; Serno,P.; Bischoff,E.; El-Sayed,M.; Niew鰄ner,U.; Nowakowski,M.; Schenke,T.; Dembowsky,K.(Bayer AG)
参考来源:DE 19750085; DE 19812462; EP 1049695; WO 9924433
📄 详细内容
合成路线:Cyclization of 2-ethoxybenzamidine (I) with 2-butyramidopropionic acid (II) and ethoxalyl chloride (III) by means of DMAP in refluxing pyridine gives 2-(2-ethoxyphenyl)-5-methyl-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-4-one (IV),which is sulfonated with chlorosulfonic acid to provide the sulfonyl chloride (V).Finally,this compound is condensed with 1-ethylpiperazine (VI) in dichloromethane.
参考文献标题:Vardenafil
文献作者:Castar,J.; Mart韓,L.; Rabasseda,X.; Sorbera,L.A.
参考来源:Drugs Fut 2001,26(2),141
合成路线:Cyclization of 2-ethoxybenzamidine (I) with 2-butyramidopropionic acid (II) and ethoxalyl chloride (III) by means of DMAP in refluxing pyridine gives 2-(2-ethoxyphenyl)-5-methyl-7-propyl-3,4-dihydroimidazo[5,1-f][1,2,4]triazin-4-one (IV),which is sulfonated with chlorosulfonic acid to provide the sulfonyl chloride (V).Finally,this compound is condensed with 1-ethylpiperazine (VI) in dichloromethane.
参考文献标题:Imidazo[5,1-f][1,2,4]triazin-4(3H)-ones,a new class of potent PDE 5 inhibitors
文献作者:Haning,H.; Niew鰄ner,U.; Schenke,T.; Es-Sayed,M.; Schmidt,G.; Lampe,T.; Bischoff,E.
参考来源:Bioorg Med Chem Lett 2002,12(6),865