Pibutidine hydrochloride, IT-066
3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮盐酸盐 3-氨基-4-[[(Z)-4-[4-(哌啶-1-基甲基)吡啶-2-基]氧基丁-2-烯基]氨基]环丁-3-烯-1,2-二酮 Chemical Name: 3-Amino-4-[4-[4-(1-piperidinylmethyl)-2-pyridyloxy]-2(Z)-butenylamino]-3-cyclobutene-1,2-dione hydrochloride
CAS No. 126463-66-9, 103922-33-4 (free base)
项目整合开发状态: Pre-Registered
项目研究机构: Ikeda Mohando (Originator), Taisho (Codevelopment)
合成路线:The condensation of 4-amino-2(Z)-buten-1-ol (I) with 2-bromo-4-(piperidinomethyl)pyridine (II) by means of NaH in refluxing THF gives 4-[4-(piperidinomethyl)pyridin-2-yloxy]-2(Z)-butenylamine (III),which is allowed to react with 3,4,-dimethoxy-3-cyclobutene-1,2-dione (IV) in methanol to afford 3-methoxy-4-[4-[4-(piperidinomethyl)pyridin-2-yloxy]-2(Z)-butenylamino]-3-cyclobutene-1,2-dione (V).Finally,this compound is treated with dry ammonia in methanol.
📌 参考资料/链接：
参考文献标题:Pyridyloxy derivs.
文献作者:Nohara,F.; Fujinawa,T.(Ikeda Mohando)
参考来源:AU 8548136; EP 0177016; ES 8701161; JP 1986085365; JP 1986207375; JP 1991261766; US 4710498
📄 详细内容
合成路线:The condensation of 4-amino-2(Z)-buten-1-ol (I) with 2-bromo-4-(piperidinomethyl)pyridine (II) by means of NaH in refluxing THF gives 4-[4-(piperidinomethyl)pyridin-2-yloxy]-2(Z)-butenylamine (III),which is allowed to react with 3,4,-dimethoxy-3-cyclobutene-1,2-dione (IV) in methanol to afford 3-methoxy-4-[4-[4-(piperidinomethyl)pyridin-2-yloxy]-2(Z)-butenylamino]-3-cyclobutene-1,2-dione (V).Finally,this compound is treated with dry ammonia in methanol.
参考文献标题:IT-066
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1990,15(12),1181
产品链接: CAS No. 126463-66-9›› 产品链接: CAS No.103922-33-4››