Vintoperol, RT-3003, RGH-2981
长春培醇Chemical Name: (-)-(1S,12bS)-1-Ethyl-1-hydroxymethyl-1,2,3,4,6,7,12,12b-octahydroindolo[2,3-a]quinolizine
CAS No. 106498-99-1, 58451-76-6 (racemate)
项目整合开发状态: Phase II
项目研究机构: Gedeon Richter (Originator), Takata Seiyaku (Licensee)
合成路线:Conversion of racemic 1-ethyl-2,3,4,6,7,10-hexahydroindolo[2,3-a] quinolizine (I),an intermediate in the synthesis of vincamine,to the base and reaction of the latter with paraformaldehyde gives the 1-hydroxymethyl compound (II),which is acetylated to give the acetate (III).(III) is separated to its enantiomers by salt formation with (+)- (2R,3R)-tartaric acid,followed by fractional crystallization.Treatment of the separated tartrates with sodium methoxide gives the optically active bases,i.e.,(+)-(II) and (-) (II) (RGH-2981).
📌 参考资料/链接：
参考文献标题:RGH-2981
文献作者:N骻r醖i,M.
参考来源:Drugs Fut 1986,11(10),853
📄 详细内容
合成路线:Conversion of racemic 1-ethyl-2,3,4,6,7,10-hexahydroindolo[2,3-a] quinolizine (I),an intermediate in the synthesis of vincamine,to the base and reaction of the latter with paraformaldehyde gives the 1-hydroxymethyl compound (II),which is acetylated to give the acetate (III).(III) is separated to its enantiomers by salt formation with (+)- (2R,3R)-tartaric acid,followed by fractional crystallization.Treatment of the separated tartrates with sodium methoxide gives the optically active bases,i.e.,(+)-(II) and (-) (II) (RGH-2981).
参考文献标题:
文献作者:Somogyi,A.; Rohner,H.-G.; Gugler,R.
参考来源:J Org Chem 1985,50(1),3760
产品链接: CAS No. 106498-99-1››