Rotraxate hydrochloride, TEI-5103, Cumelon
Chemical Name: trans-4-[[4-(Aminomethyl)cyclohexyl]carbonyl]benzenepropanoic acid hydrochloride; 3-[p-(trans-4-Aminomethylcyclohexylcarbonyl)phenyl]propionic acid hydrochloride
CAS No. 82085-94-7
项目整合开发状态: Phase III
项目研究机构: Teijin (Originator)
合成路线:This compound can be obtained by two different ways:1) The Friedel Crafts' condensation of trans-4-aminomethylcyclohexylcarbonyl chloride (I) with methyl 3-phenylpropionate (II) by means of AlCl3 in refluxing S2C gives methyl 3-[4-trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionate (III),which is then hydrolyzed with hot aqueous concentrated HCl.2) By isomerization of 3-[4-(cis-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid (IV) in hot aqueous 3N HCl.
📌 参考资料/链接：
参考文献标题:Aminocarboxylic acids,amino alcohols or the derivatives thereof,processes for production thereof and pharmaceutical uses thereof
文献作者:Takeshita,T.; Hoshina,K.; Ohtsu,A.; Naruchi,T.(Teijin Ltd.)
参考来源:CA 1176267; EP 0044541; US 4402975
📄 详细内容
合成路线:This compound can be obtained by two different ways:1) The Friedel Crafts' condensation of trans-4-aminomethylcyclohexylcarbonyl chloride (I) with methyl 3-phenylpropionate (II) by means of AlCl3 in refluxing S2C gives methyl 3-[4-trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionate (III),which is then hydrolyzed with hot aqueous concentrated HCl.2) By isomerization of 3-[4-(cis-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid (IV) in hot aqueous 3N HCl.
参考文献标题:TEI-5103
文献作者:Castar,J.; Serradell,M.N.
参考来源:Drugs Fut 1985,10(6),485
合成路线:This compound can be obtained by two different ways:1) The Friedel Crafts' condensation of trans-4-aminomethylcyclohexylcarbonyl chloride (I) with methyl 3-phenylpropionate (II) by means of AlCl3 in refluxing S2C gives methyl 3-[4-trans-4-aminomethylcyclohexylcarbonyl)phenyl]propionate (III),which is then hydrolyzed with hot aqueous concentrated HCl.2) By isomerization of 3-[4-(cis-4-aminomethylcyclohexylcarbonyl)phenyl]propionic acid (IV) in hot aqueous 3N HCl.
参考文献标题:
文献作者:Verloes,R.; Delire,M.; Brichard,V.; Portielje,J.P.; Stoter,G.; Kruit,W.H.J.; van Ojik,H.H.
参考来源:Drugs Today 1980,16(9),290
产品链接: CAS No. 82085-94-7››