Pirodavir, R-77975
吡罗达韦Chemical Name: 4-[2-[1-(6-Methyl-3-pyridazinyl)-4-piperidinyl]ethoxy]benzoic acid ethyl ester
CAS No. 124436-59-5
项目整合开发状态: Phase II
项目研究机构: Janssen (Originator)
合成路线:The condensation of 2-(1-benzylpiperidin-4-yl)ethanol (I) with 4-hydroxybenzoic acid ethyl ester (II) by means of triphenylphosphine and diazenedicarboxylic acid diethyl ester in THF gives 4-[2-(1-benzylpiperidin-4-yl)ethoxy]benzoic acid ethyl ester (III) as fumarate salt.This compound is debenzylated by hydrogenation with H2 over Pd/C in ethanol,yielding the free product (IV),which is finally condensed with 3-chloro-6-methylpyridazine (V) by means of K2CO3 in DMF.
📌 参考资料/链接：
参考文献标题:Novel pyridazinamine derivs
文献作者:Stokbroekx,R.A.; Van der Aa,M.J.M.; Luyckx,M.G.M.; Grauwels,G.A.J.(Janssen Pharmaceutica NV)
参考来源:AU 8825751; EP 0320032; JP 1989207278; US 4992433
📄 详细内容
合成路线:The condensation of 2-(1-benzylpiperidin-4-yl)ethanol (I) with 4-hydroxybenzoic acid ethyl ester (II) by means of triphenylphosphine and diazenedicarboxylic acid diethyl ester in THF gives 4-[2-(1-benzylpiperidin-4-yl)ethoxy]benzoic acid ethyl ester (III) as fumarate salt.This compound is debenzylated by hydrogenation with H2 over Pd/C in ethanol,yielding the free product (IV),which is finally condensed with 3-chloro-6-methylpyridazine (V) by means of K2CO3 in DMF.
参考文献标题:Pirodavir
文献作者:Castar,J.; Prous,J.
参考来源:Drugs Fut 1992,17(11),997
产品链接: CAS No. 124436-59-5››