BAY-58-2667

4-N-(4-羧基丁基)-N-2-2-4-(2-苯基乙基)苄氧基苯基乙基氨基甲基苯甲酸Chemical Name: 4-[N-(4-Carboxybutyl)-N-[2-[2-[4-(2-phenylethyl)benzyloxy]phenyl]ethyl]aminomethyl]benzoic acid
CAS No. 329773-35-5
项目整合开发状态: Preclinical
项目研究机构: Bayer (Originator)
合成路线:2-Methoxyphenethylamine (I) is condensed with methyl 4-formylbenzoate (II) to form imine (III),which is further reduced to amine (IV) with NaBH4 in MeOH.Alkylation of amine (IV) by ethyl 5-bromovalerate (V) affords the amino diester (VI).Methyl ether cleavage in (VI) by means of BBr3 gives rise to the phenol compound (VII),which is alkylated with 4-(chloromethyl)stilbene (VIII) to yield ether (IX).Catalytic hydrogenation of stilbene (IX) yields the phenethylbenzyl derivative (X).Finally,alkaline hydrolysis of the methyl ester groups of (X) leads to the title dicarboxylic acid.
📌 参考资料/链接:
参考文献标题:Novel derivs.of dicarboxylic acid having pharmaceutical properties
文献作者:Perzborn,E.; Stasch,J.-P.; Heil,M.; Naab,P.; Dembowsky,K.; Alonso-Alija,C.; Stahl,E.; Pernerstorfer,J.; Flubacher,D.; Wunder,F.(Bayer AG)
参考来源:DE 19943635; EP 1216225; WO 0119780

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