A-176120
5-[N-(2-乙氧基苯甲基)-N-[3-(4-甲基苯氧基)苯甲基]氨基甲酰]-1,2,4-苯三羧酸Chemical Name: 5-[N-(2-Ethoxybenzyl)-N-[3-(4-methylphenoxy)benzyl]carbamoyl]-1,2,4-benzenetricarboxylic acid
CAS No. 185049-54-1
项目整合开发状态: Preclinical
项目研究机构: Abbott (Originator)
合成路线:Reaction of 4-methylphenol (I) with NaH in DMF and 3-fluorobenzaldehyde (II) yields aldehyde (III),which will be converted into secondary amine (V) via a reductive amination with amine (IV) in presence of NaBH3CN in MeOH and catalytic HOAc.Amine (V) couples with dianhydride (VI) in THF in presence of NMM or alternatively in toluene and Et3N.Final treatment with Na2CO3 in THF yields the desired product.
📌 参考资料/链接：
参考文献标题:Benzene,pyridine,naphthalene or benzophenone derivs.as inhibitors of squalene synthetase and protein farnesyltransferase
文献作者:Sullivan,G.M.; Rosenberg,S.H.; Prasad,R.N.; O'Connor,S.J.; Donner,B.G.; Fakhoury,S.A.; Fung,K.L.; Stout,D.M.; Rockway,T.W.; Baker,W.R.; Shen,W.; Garvey,D.S.(Abbott Laboratories Inc.)
参考来源:WO 9634851