Proglumetacin maleate, Protaxon, Proxil
Chemical Name: 4-Benzamido-5-(dipropylamino)-5-oxopentanoic acid 3-[4-[2-[2-[1-(4-chlorobenzoyl)-5-methoxy-2-methyl-1H-indol-3-yl]acetoxy]ethyl]piperazin-1-yl]propyl ester dimaleate
项目整合开发状态: Launched
项目研究机构: Opfermann Arzneimittel (Originator), Rotta (Originator)
合成路线:The reaction of N-benzoyl-N?N?di-n-propyl-DL-isoglutamine (I) with N-3-chloropropyl-N?2-hydroxyethylpiperazine (II) by means of sodium methoxide in DMSO at 105 C gives N-[3-(N-benzoyl-N?N?di-n-propyl-DL-isoglutaminyl)oxypropyl]-N?(2-hydroxyethyl)piperazine (III),which is then condensed with 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid (IV) by means of dicyclohexylcarbodiimide and NaHCO3 in ethyl acetate,and treated finally with maleic acid (V)
📌 参考资料/链接：
参考文献标题:Proglumetacin maleate
文献作者:Blancafort,P.; Serradell,M.N.; Casta馿r,J.; de Angelis,L.
参考来源:Drugs Fut 1980,5(3),142
📄 详细内容
合成路线:The reaction of N-benzoyl-N?N?di-n-propyl-DL-isoglutamine (I) with N-3-chloropropyl-N?2-hydroxyethylpiperazine (II) by means of sodium methoxide in DMSO at 105 C gives N-[3-(N-benzoyl-N?N?di-n-propyl-DL-isoglutaminyl)oxypropyl]-N?(2-hydroxyethyl)piperazine (III),which is then condensed with 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetic acid (IV) by means of dicyclohexylcarbodiimide and NaHCO3 in ethyl acetate,and treated finally with maleic acid (V)
参考文献标题:
文献作者:Makovec,F.; et al.(Rotta Research Laboratorium SpA)
参考来源:BE 830880; CA 1053663; DE 2535799; FR 2281755; GB 1467568; JP 7643773; JP 7643774; JP 7916511; JP 7916512; NL 7509091; SA 7509091; US 3985878