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新产品编号:2028633

Chemical Name: 3,4,5-Trimethoxybenzoic acid 2,4-diaminoquinazolin-6-ylmethyl ester
项目整合开发状态: Preclinical
项目研究机构: Melacure Therapeutics (Originator)
合成路线:Nitrile (II) was prepared by regioselective diazotization of triaminoquinazoline (I),followed by treatment with KCN and CuSO4.Conversion of nitrile (II) into aldehyde (III) was achieved by means of Ni-Al alloy in refluxing formic acid.Subsequent reduction of aldehyde (III) with NaBH4 gave alcohol (IV),which was further brominated to (V) using HBr in HOAc.Finally,displacement of the bromide of (V) with 3,4,5-trimethoxybenzoic acid (VI) provided the target trimethoxybenzoate ester.
📌 参考资料/链接:
参考文献标题:Design,synthesis,computational prediction,and biological evaluation of ester soft drugs as inhibitors of dihydrofolate reductase from Pneumocystis carinii
文献作者:Graffner-Nordberg,M.; Kolmodin,K.; Aqvist,J.; Queener,S.F.; Hallberg,A.
参考来源:J Med Chem 2001,44(15),2391