Microwave Assisted Synthesis And Anti-Hiv-Rt Activity Of Diary! Benzo[1,3]Thiazin-4-Ones

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-dichloropheny1)-3-(4,6-di-methylpyrimidin-2-yl)-2H-benzo[e][1,3]thiazin-4(3.H)-one (10c) could effectively inhibit HIV-RT activity with the IC50 value of 8.38 mu mol.L-1, the others showed middle RT inhibitory activity.