CDRI-93/478
Chemical Name: 1-[3-[4-(4-Fluorophenyl)piperazin-1-yl]propyl]pyrrolidin-2-one hydrochloride
CAS No. 223525-77-7 (free base)
项目整合开发状态: Preclinical
项目研究机构: Central Drug Research Institute (Originator), Council Scientific Ind. Res. (Originator)
合成路线:The title compound was synthesized by two related methods.2-Pyrrolidone (I) was alkylated with 1-bromo-3-chloropropane (II) using either sodium or potassium metal or potassium tert-butoxide as the base.The resultant N-(3-chloropropyl)pyrrolidone (III) was then condensed with 1-(4-fluorophenyl)piperazine (IV) in the presence of NaI and Na2CO3 to produce the desired disubstituted piperazine.Alternatively,the title compound was prepared from the known N-(3-chloropropyl)-N'-(4-fluorophenyl)piperazine (V) by condensation with 2-pyrrolidone (I) in the presence of sodium metal in hot xylene.
📌 参考资料/链接:
参考文献标题:1-[4-Arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes and their use in medical treatments
文献作者:Jain,S.; Sinha,N.; Saxena,A.K.; Anand,N.; Saxena,R.M.; Dubey,M.P.; Patnaik,G.K.; Ray,M.(Council of Scientific and Industrial Research)
参考来源:US 6150367
📄 详细内容
合成路线:The title compound was synthesized by two related methods.2-Pyrrolidone (I) was alkylated with 1-bromo-3-chloropropane (II) using either sodium or potassium metal or potassium tert-butoxide as the base.The resultant N-(3-chloropropyl)pyrrolidone (III) was then condensed with 1-(4-fluorophenyl)piperazine (IV) in the presence of NaI and Na2CO3 to produce the desired disubstituted piperazine.Alternatively,the title compound was prepared from the known N-(3-chloropropyl)-N'-(4-fluorophenyl)piperazine (V) by condensation with 2-pyrrolidone (I) in the presence of sodium metal in hot xylene.
参考文献标题:Methods for preparing 1-[4-arylpiperazin-1-yl]-3-[2-oxopyrrolidin/piperidin-1-yl]propanes
文献作者:Jain,S.; Sinha,N.; Saxena,A.K.; Anand,N.; Saxena,R.M.; Dubey,M.P.; Patnaik,G.K.; Ray,M.(Council of Scientific and Industrial Research)
参考来源:US 6084097