Rasagiline mesilate, TVP-1012, (+)-AGN-1135, Agilect
甲磺酸雷沙吉兰 雷沙吉兰 Chemical Name: 1(R)-(Propargylamino)indane methanesulfonate; 1(R)-(2-Propynylamino)indane methanesulfonate; (R)-N-2-Propynyl-1-indanamine methanesulfonate
CAS No. 161735-79-1, 136236-51-6 (free base)
项目整合开发状态: Pre-Registered
项目研究机构: Teva (Originator), Lundbeck (Licensee), Eisai (Codevelopment)
合成路线:Rasagiline can be obtained by two related ways:1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III),which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10).2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.
📌 参考资料/链接：
参考文献标题:R-Enantiomers of N-propargyl-1-aminoindan cpds.,their preparation and pharmaceutical compsns.containing them
文献作者:Youdim,M.B.H.; Finberg,J.P.M.; Levy,R.; Sterling,J.; Lerner,D.; Berger-Paskin,T.(Teva Pharmaceutical Industries Ltd.)
参考来源:EP 0436492; JP 1991294248; US 5453446
📄 详细内容
合成路线:Rasagiline can be obtained by two related ways:1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III),which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10).2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.
参考文献标题:R-Enantiomer of N-propargyl-1-aminoindan,salts,compsns.and uses thereof
文献作者:Youdim,M.B.H.; Finberg,J.P.M.; Levy,R.; Sterling,J.; Lerner,D.; Berger-Paskin,T.; Yellin,H.; Veinberg,A.(Teva Pharmaceutical Industries Ltd.)
参考来源:WO 9511016
合成路线:Rasagiline can be obtained by two related ways:1) The alkylation of racemic 1-aminoindane with propagyl chloride (II) and K2CO3 in hot acetonitrile gives the racemic secondary amine (III),which is submitted to optical resolution by chromatography over Chiracel OJ and eluting with hexane/isopropanol (90:10).2) By alkylation of (R)-1-aminoindane (IV) with propargyl chloride (or bromide) (II) as before.
参考文献标题:Rasagiline
文献作者:Graul,A.; Castar,J.
参考来源:Drugs Fut 1996,21(9),903
产品链接: CAS No. 161735-79-1›› 产品链接: CAS No.136236-51-6››