Synthesis of substituted novel quinazolinone compounds

ZHAO Lei; ZHAO Xuemei; TANG Hui; WU Juan

doi:10.3969/j.issn.1006-0111.2015.06.013

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Objective To optimize the synthesis route of substituted quinazolinone and investigate the influence of temperature and time in the synthesis of key intermediates. Methods A parallel test was carried out to compare temperature, time and the ester bond ammonolysis of condensing agent, including the total analysis of experimental result. And orthogonal experimental design was used and the influence of temperature and time on the yield were investigated. Results and Conclusion The structure of the compound was confirmed by ¹H NMR, MS and ¹³C NMR. When the reaction temperature was 30 ℃, the reaction time was 24 h with the condensing agent (DCC) and the reactant ratio of 1.5:1, the yield of ester bond ammonolysis was higher. The optimal preparation procedure of quinazolinone compounds was more available for industrial production. In vitro antifungal activity test Results showed that the lead compounds measured on five clinical pathogenic fungi have the potential antifungal activity, and are worth for further study.

Synthesis of substituted novel quinazolinone compounds

1. Shandong Provincial Hospital affiliated to Shandong University, Jinan 250021, China;Qilu Hospital of Shandong University, Jinan 250012, China

2. Shandong Provincial Hospital affiliated to Shandong University, Jinan 250021, China

3. Chengdu Military General Hospital, Chengdu 610083, China

Received Date: 2014-05-19

Rev Recd Date: 2014-11-06

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Abstract: Objective To optimize the synthesis route of substituted quinazolinone and investigate the influence of temperature and time in the synthesis of key intermediates. Methods A parallel test was carried out to compare temperature, time and the ester bond ammonolysis of condensing agent, including the total analysis of experimental result. And orthogonal experimental design was used and the influence of temperature and time on the yield were investigated. Results and Conclusion The structure of the compound was confirmed by ¹H NMR, MS and ¹³C NMR. When the reaction temperature was 30 ℃, the reaction time was 24 h with the condensing agent (DCC) and the reactant ratio of 1.5:1, the yield of ester bond ammonolysis was higher. The optimal preparation procedure of quinazolinone compounds was more available for industrial production. In vitro antifungal activity test Results showed that the lead compounds measured on five clinical pathogenic fungi have the potential antifungal activity, and are worth for further study.

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Reference (13)

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Synthesis of substituted novel quinazolinone compounds

doi: 10.3969/j.issn.1006-0111.2015.06.013

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通讯作者: 陈斌, [email protected]

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