Quinazoline antifolate thymidylate synthase inhibitors: difluoro-substituted benzene ring analogs

…, AL Jackman, PR Marsham, BM O'Connor…

文献索引：Thornton; Jackman; Marsham; O'Connor; Bishop; Calvert Journal of Medicinal Chemistry, 1992 , vol. 35, # 12 p. 2321 - 2327

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被引用次数: 10

摘要

The syntheeis of a aeries of new Cn-methyl-Wo-aJkylquinamline-based thymidylate synthase (TS) inhibitora containing difluorinated p-aminobenzoate rings is described. Derivatives of the Mo-propargyl and No-methylquinazoline antjfolatea were prepared with 2', 3'-, 2', 5'-, and 2", 6'-difluon, subatitution. The syntheaia of the 2', S'-difluon, analogues involved oxidation of the difluoronitrotoluene to 2, bdMuoro-4-nitrobem0ic acid followed ...