TRM-115
Chemical Name: 4-[3-(Benzo-1,3-dioxol-5-yl)thioureido]-N-[3-[3-(piperidinomethyl)phenoxy]propyl]butyramide; 1-[3-[N-[3-[3-(Piperidinomethyl)phenoxy]propyl]carbamoyl]propyl]-3-[(3,4-methylenedioxy)phenyl]thiourea
CAS No. 147779-46-2
项目整合开发状态: Phase I
项目研究机构: Terumo (Originator)
合成路线:The condensation of gamma-aminobutylic acid (I) with 3,4-methylenedioxyphenylisothiocyanate (II) in ethanol-H2O gives 1-[3-(carboxy)propyl]-3-(3,4-methylenedioxyphenyl)thiourea (III),which is allowed to react with 3-[3-(piperidinomethyl)phenoxy]propylamine (IV) by means of ethyl chloroformate and triethylamine in dichloromethane to afford TRM-115.
📌 参考资料/链接：
参考文献标题:Synthesis of TRM-115,a new antiulcer agent,and its pharmacological action
文献作者:Matsushima,H.; Nanba,R.; Isozaki,M.; Nakazawa,K.; Koyama,S.
参考来源:113th Annu Meet Pharmaceut Soc Jpn (March 29-31,Osaka) 1993,Abst 29PB 13-04.
📄 详细内容
合成路线:The condensation of gamma-aminobutylic acid (I) with 3,4-methylenedioxyphenylisothiocyanate (II) in ethanol-H2O gives 1-[3-(carboxy)propyl]-3-(3,4-methylenedioxyphenyl)thiourea (III),which is allowed to react with 3-[3-(piperidinomethyl)phenoxy]propylamine (IV) by means of ethyl chloroformate and triethylamine in dichloromethane to afford TRM-115.
参考文献标题:TRM-115
文献作者:Takenaga,T.; Isozaki,M.
参考来源:Drugs Fut 1993,18(10),909
合成路线:The condensation of gamma-aminobutylic acid (I) with 3,4-methylenedioxyphenylisothiocyanate (II) in ethanol-H2O gives 1-[3-(carboxy)propyl]-3-(3,4-methylenedioxyphenyl)thiourea (III),which is allowed to react with 3-[3-(piperidinomethyl)phenoxy]propylamine (IV) by means of ethyl chloroformate and triethylamine in dichloromethane to afford TRM-115.
参考文献标题:Synthesis of TRM-115
文献作者:Isozaki,M.; Nakazawa,K.; Nanba,R.; Matsushima,H.; Koyama,S.
参考来源:Terumo Co.,Ltd.Internal Report
合成路线:The condensation of gamma-aminobutylic acid (I) with 3,4-methylenedioxyphenylisothiocyanate (II) in ethanol-H2O gives 1-[3-(carboxy)propyl]-3-(3,4-methylenedioxyphenyl)thiourea (III),which is allowed to react with 3-[3-(piperidinomethyl)phenoxy]propylamine (IV) by means of ethyl chloroformate and triethylamine in dichloromethane to afford TRM-115.
参考文献标题:Thiourea derivs
文献作者:Nakazawa,K.; Isozaki,M.; Koyama,S.(Terumo Corp.)
参考来源:JP 93059038