Cetraxate hydrochloride, DV-1006, Neuer
Chemical Name: trans-3-[4-[4-(Aminomethyl)cyclohexylcarbonyloxy]phenyl]propionic acid hydrochloride
项目整合开发状态: Launched
项目研究机构: Daiichi Pharmaceutical (Originator)
合成路线:By condensation of trans-4-toluenesulfonylaminomethylcyclohexane carbonyl chloride (I) and benzyl 4-hydroxyphenylpropionate (II) by means of Et3N and hot benzene followed by debenzylation using H2 over Pd/C in AcOH.
合成路线:By condensation of trans-4-cyanocyclohexanecarbonyl chloride (III) and the benzyl ester (II) by means of triethylamine in hot benzene followed by debenzylation using H2 over Pd/C in acetic acid giving the cyanoester (IV),which is then reduced with H2 over Raney-Ni in ethyl acetate - ethanol - water.
📌 参考资料/链接：
参考文献标题:Medicinal chemical studies on antiplasmin drugs.4.Chemical modification of trans-4-aminomethylcyclohexacarboxylic acid and its effect on antiplasmin activity
文献作者:Okano,A.; Inaoka,M.; Funabashi,S.; Iwamoto,M.; Isoda,S.
参考来源:J Med Chem 1972,15(3),247-255
📄 详细内容
合成路线:By condensation of trans-4-toluenesulfonylaminomethylcyclohexane carbonyl chloride (I) and benzyl 4-hydroxyphenylpropionate (II) by means of Et3N and hot benzene followed by debenzylation using H2 over Pd/C in AcOH.
参考文献标题:
文献作者:Kitahara,S.
参考来源:JP 48075547
合成路线:By condensation of trans-4-toluenesulfonylaminomethylcyclohexane carbonyl chloride (I) and ter-butyl-4-hydroxyphenylpropionate (V) and performing the hydrolysis with HCl - acetic acid at room temperature.
参考文献标题:
文献作者:Kitahara,S.
参考来源:JP 48078143
合成路线:By condensation of trans-4-toluenesulfonylaminomethylcyclohexane carbonyl chloride (I) and benzyl 4-hydroxyphenylpropionate (II) by means of Et3N and hot benzene followed by debenzylation using H2 over Pd/C in AcOH.
合成路线:By condensation of trans-4-cyanocyclohexanecarbonyl chloride (III) and the benzyl ester (II) by means of triethylamine in hot benzene followed by debenzylation using H2 over Pd/C in acetic acid giving the cyanoester (IV),which is then reduced with H2 over Raney-Ni in ethyl acetate - ethanol - water.
合成路线:By condensation of trans-4-toluenesulfonylaminomethylcyclohexane carbonyl chloride (I) and ter-butyl-4-hydroxyphenylpropionate (V) and performing the hydrolysis with HCl - acetic acid at room temperature.
参考文献标题:Cetraxate
文献作者:Roberts,P.J.; Casta馿r,J.
参考来源:Drugs Fut 1977,2(8),504