【摘 要】
：
以2-氨基-4-硝基-苯甲酸和醋酸甲脒为原料,合成了7-硝基-喹唑啉酮(3),化合物3在SOCl2的作用下氯代得7-硝基-4-氯-喹唑啉(4);又以取代苯甲醛为起始原料,通过合成肟、1,3偶极环
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以2-氨基-4-硝基-苯甲酸和醋酸甲脒为原料,合成了7-硝基-喹唑啉酮(3),化合物3在SOCl2的作用下氯代得7-硝基-4-氯-喹唑啉(4);又以取代苯甲醛为起始原料,通过合成肟、1,3偶极环加成反应、甲磺酰化、叠氮化、Zn/NH4Cl还原得中间体3-(取代苯基)-异噁唑-5-甲胺衍生物5a～5e.4与5a～5e在碱性氧化铝作用下固相研磨合成了5种未见文献报道的新型的含异噁唑环的喹唑啉衍生物6a～6e.所合成的化合物通过IR,1HNMR,MS等分析方法进行了表征.体外抑蛋白酪氨酸酶α(PTPα)和蛋白酪氨酸酶ε(PTPε)活性测试结果表明测试样品浓度在20μg/mL下对PTPα和PTPε均无显著的抑制活性.
Nitro-quinazolinone (3) was synthesized from 2-amino-4-nitro-benzoic acid and formamidine acetate. Compound 3 was chlorinated with SOCl2 to give 7-nitro- - chloro-quinazoline (4). The substituted benzaldehyde was used as the starting material to synthesize the intermediate of oxime, 1,3-dipolar cycloaddition reaction, mesylation, azidation and Zn / NH4Cl reduction 5-isoxazol-5-methylamine Derivatives 5a-5e.4 and 5a-5e were synthesized by solid-state milling with basic alumina. Quinazoline derivatives 6a to 6e of the oxazole ring The synthesized compounds were characterized by IR, 1HNMR, MS, etc. In vitro, the protein tyrosinase α (PTPα) and protein tyrosinase ε (PTPε ) Activity test results show that the test sample concentration of 20μg / mL PTPα and PTPε no significant inhibitory activity.
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