8-羧基喹唑啉酮衍生物的合成

Synthesis of 8-Carboxyquinazolinone Derivatives

以2-氨基-3-甲基苯甲酸为起始原料,经醋酸酐乙酰化、氧化、关环、取代等反应,设计合成了一系列8-羧基-2-甲基-3-芳基(脂肪基)-4(3H)-喹唑啉酮衍生物,所有目标化合物均测定了熔点并通过了1H NMR和质谱结构表征。通过单晶结构测试,发现该类化合物存在很强的氢键,很难进一步酯化或合成酰胺。

The synthesize route of 2-methyl-4-oxo-3-phenyl-3,4-dihydroquinazoline-8-carboxylic acid derivatives undergoed acetylation,oxidation,cyclization and substitution reactions from the starting material of 2-amino-3-methylbenzoic acid.All of the target compounds were confirmed by ~1 HNMR,MS and melting point.According to the result of X-ray diffraction analysis,this series compounds existed strong hydrogen bond that was very difficult for further reaction of esterification or amidation.