新产品编号:2041289
Chemical Name: N-[3-(7-Chloroquinolin-4-ylamino)-5-(morpholin-4-ylmethyl)phenyl]-2-(1-piperidinyl)acetamide
项目整合开发状态: Preclinical
项目研究机构: CNRS (Originator), Tibotec-Virco (Originator)
合成路线:The intermediate anilinoquinoline (III) was obtained by nucleophilic substitution of 4,7-dichloroquinoline (II) with 3,5-diaminobenzyl alcohol (I) in the presence of N-methylmorpholine.Coupling of (III) with chloroacetic acid gave the corresponding chloroacetamide (IV),which was further reacted with piperidine in DMF,yielding the piperidino acetamide (V).The benzyl alcohol function of (V) was then oxidized to aldehyde (VI) employing manganese dioxide.Finally,reductive condensation of aldehyde (VI) with morpholine in the presence of NaBH(OAc)3 furnished the title compound.
📌 参考资料/链接:
参考文献标题:Synthesis and in vitro and in vivo antimalarial activity of new 4-anilinoquinolines
文献作者:Delareu,S.; Girault,S.; Maes,L.; Debreu-Fontaine,M.A.; Labaeid,M.; Grellier,P.; Sergheraert,C.
参考来源:J Med Chem 2001,44(17),2827