6-喹唑啉酮甲酯衍生物的合成研究

Synthesis of 6-Carboxyquinazolinone Derivatives

喹唑啉酮及其衍生物是一类具有广泛生物活性的化合物。本文以2,4-二甲基苯胺为起始原料,经乙酰化、氧化、甲酯化、关环、取代等反应,设计合成了一系列新型的6-甲酯-2-氯甲基(或三氟甲基)-3-芳基-4-喹唑啉酮衍生物,所有目标化合物均测定了熔点,并用1H-NMR和质谱进行结构表征。进一步实验发现,该喹唑啉酮衍生物很难通过水解的方法得到相应的羧酸。

Quinazolinone and its derivatives often display excellent bio-activities. The synthesize route of methyl 2-（ chloromethyl or trifluoromethyl）-3-（ phenyl）-4-oxo-quinazoline-6-carboxylate derivatives was undergone acetylation,oxidation,methylation,cyclization and substitution reactions from the starting 2,4-dimethylaniline. All of the target compounds were confirmed by1 HNMR,MS and melting point. These series compounds were very difficult for further reaction of hydrolysis to get corresponding carboxylic acid.