Blonanserin, AD-5423, Lonasen
布南色林Chemical Name: 2-(4-Ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydrocycloocta[b]pyridine
CAS No. 132810-10-7
项目整合开发状态: Phase III
项目研究机构: Dainippon Pharmaceutical (Originator), Almirall Prodesfarma (Licensee)
合成路线:The condensation of cyclooctanone (I) with 4-fluorobenzoylacetonitrile (II) by heating with polyphosphoric acid at 120 C gives 4-fluorophenyl-5,6,7,8,9,10-hexahydrocycloocta[b]pyridin-2(1H)-one (III),which is converted to the corresponding 2-chloro derivative (IV) by treatment with refluxing phosphoryl chloride.The reaction of (IV) with 1-ethylpiperazine (V) at 170 C affords AD-5423.
📌 参考资料/链接：
参考文献标题:2-(1-Piperazinyl)-4-phenylcycloalkanopyridine derivs.,processes for the production thereof,and pharmaceutical compsn.containing the same
文献作者:Hino,K.; Kai,N.; Sakamoto,M.; Kon,T.; Oka,M.; Furakawa,K.; Ochi,Y.(Dainippon Pharmaceutical Co.,Ltd.)
参考来源:EP 0385237; JP 1991007257; JP 1994041079; US 5021421
📄 详细内容
合成路线:The condensation of cyclooctanone (I) with 4-fluorobenzoylacetonitrile (II) by heating with polyphosphoric acid at 120 C gives 4-fluorophenyl-5,6,7,8,9,10-hexahydrocycloocta[b]pyridin-2(1H)-one (III),which is converted to the corresponding 2-chloro derivative (IV) by treatment with refluxing phosphoryl chloride.The reaction of (IV) with 1-ethylpiperazine (V) at 170 C affords AD-5423.
参考文献标题:AD-5423
文献作者:Oka,M.; Hino,K.
参考来源:Drugs Fut 1992,17(1),9
产品链接: CAS No. 132810-10-7››