Chinese Journal of Organic Chemistry >
Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones
Received date: 2014-12-30
Revised date: 2015-02-03
Online published: 2015-02-05
Supported by
Project supported by the National Natural Science Foundation of China (No. 21372060), the Medicinal Joint Funds of the Natural Science Foundation of Hebei and Shijiazhuang Pharmaceutical Group (No. B2012201113), the Natural Science Foundations of Education Department of Hebei (No. Y2011119), and the Foundations of Baoding City Science and Technology Bureau (No. 14ZF095).
A series of novel diaryl benzothiazin-4-ones were designed and synthesized by the three-component one-pot cyclocondensation of pyrimidinamine, aromatic aldehyde and thiosalicylic acid under microwave irradiation for 10 min. The reaction has the advantages such as short reaction time and simple operation. The structures of the newly synthesized compounds were confirmed by IR, NMR, MS spectra and elemental analysis. The compound 2-(2,6-dichlorophenyl)-3-(4,6-di- methylpyrimidin-2-yl)-2H-benzo[e][1,3]thiazin-4(3H)-one (10c) could effectively inhibit HIV-RT activity with the IC50 value of 8.38 祄ol·L-1, the others showed middle RT inhibitory activity.
Key words： benzothiazin-4-one; anti-HIV-RT activity; microwave irradiation
Feng Junna , Li Xiaohui , Shao Jie , Zhu Mo , Li Yan , Chen Hua , Li Xiaoliu . Microwave Assisted Synthesis and Anti-HIV-RT Activity of Diaryl Benzo[1,3]thiazin-4-ones[J]. Chinese Journal of Organic Chemistry, 2015 , 35(6) : 1370 -1374 . DOI: 10.6023/cjoc201412053
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