Stobadine, DP-1031(dipalmitate), DH-1011(diHCl), Stobadin

2,3,4,4a,5,9b-六氢-2,8-二甲基-1h-吡嘧啶4,3-二盐酸犰酮,cisChemical Name: (-)-cis-2,3,4,4a,5,9b-Hexahydro-2,8-dimethyl-1H-pyrido[4,3-b]indole; (-)-cis-3,6-Dimethyl-1,2,3,4,4a,9a-hexahydrocarboline
CAS No. 95751-51-2
项目整合开发状态: Phase II
项目研究机构: Slovak Academy of Sciences (Originator)
合成路线:Stobadine is obtained in a 3-step synthesis including the resolution of one of the enantiomers (V)Treatment of p-tolylhydrazine (I) with N-methyl-4-piperidone (II) yields 2,8-dimethyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole (III).After catalytic hydrogenation of (III),the (?-cis isomer (IV) is obtained.In the following phase the resolution of (IV) is carried out with (+)-dibenzyoltartaric acid.After several recrystallizations,the optically pure (-)-cis-enantiomer is obtained.Treatment of the optically pure base with hydrochloric or another acid yields the corresponding salts.