Adatanserin hydrochloride, WAY-SEB-324, SEB-324, Wy-50324
阿达色林 Chemical Name: N-[2-[4-(2-Pyrimidinyl)piperazin-1-yl]ethyl]adamantane-1-carboxamide hydrochloride; N-[2-[4-(2-Pyrimidinyl)-1-piperazinyl]ethyl]tricyclo[3.3.1.1(3,7)]decane-1-carboxamide hydrochloride
CAS No. 127266-75-5 (diHCl), 127266-56-2 (free base), 144966-96-1 (monoHCl)
项目整合开发状态: Phase II
项目研究机构: Wyeth Pharmaceuticals (Originator)
合成路线:Adamantane-1-carboxylic acid chloride (freshly prepared from the reaction of thionyl chloride (I) with the adamantane-1-carboxylic acid) was reacted with 1-(2-aminoethyl)-4-(2-pyrimidinyl)piperazine (II) in CH2Cl2 in the presence of triethylamine (TEA) to afford Wy-50,324 free base in 70% (III) yield which was converted to the hydrochloride salt using ethanolic HCl solution.
📌 参考资料/链接：
参考文献标题:Aryl- and heteroaryl piperazinyl carboxamides having CNS activity
文献作者:Abou-Gharbia,M.A.-M.; Yardley,J.P.; Childers,W.E.Jr.(American Home Products Corp.)
参考来源:AU 8935025; EP 0343961; JP 1990015059
📄 详细内容
合成路线:Adamantane-1-carboxylic acid chloride (freshly prepared from the reaction of thionyl chloride (I) with the adamantane-1-carboxylic acid) was reacted with 1-(2-aminoethyl)-4-(2-pyrimidinyl)piperazine (II) in CH2Cl2 in the presence of triethylamine (TEA) to afford Wy-50,324 free base in 70% (III) yield which was converted to the hydrochloride salt using ethanolic HCl solution.
参考文献标题:Wy-50,324
文献作者:Abou-Gharbia,M.; Moyer,J.A.
参考来源:Drugs Fut 1990,15(11),1093
合成路线:Adamantane-1-carboxylic acid chloride (freshly prepared from the reaction of thionyl chloride (I) with the adamantane-1-carboxylic acid) was reacted with 1-(2-aminoethyl)-4-(2-pyrimidinyl)piperazine (II) in CH2Cl2 in the presence of triethylamine (TEA) to afford Wy-50,324 free base in 70% (III) yield which was converted to the hydrochloride salt using ethanolic HCl solution.
参考文献标题:Synthesis and SAR of adatanserin: Novel adamantyl aryl- and heteroarylpiperazines with dual serotonin 5-HT1A and activity as potential anxiolytic and antidepressant agents
文献作者:Abou-Gharbia,M.A.; Childers,W.E.Jr.; Fletcher,H.; McGaughey,G.; Patel,U.; Webb,M.B.; Yardley,J.; Andree,T.; Boast,C.; Kucharik,R.J.Jr.; Marquis,K.; Morris,H.; Scerni,R.; Moyer,J.A.
参考来源:J Med Chem 1999,42(25),5077
产品链接: CAS No.127266-56-2›› 产品链接: CAS No.144966-96-1››