Synthesis and anti-HBV activity of 2-(methylthio)thieno[3,2-d]pyrimidin-4(1H)-one analogues of ACV

Abstract

Amino thiophenecarboxylates 1a-d were heated with thiourea to afford 2-thioxothieno[3,2-d]pyrimidin-4(1H)-ones 2a-d. 2-(Methylthio)thieno[3,2-d]pyrimidin-4(1H)-ones 3a-d were synthesized by alkylation of substituted 2-thioxo derivatives 2a-d with methyl iodide. Compounds 3a-d were treated with (2-acetoxyethoxy)methyl bromide to afford 4a-d which were deacetylated to afford 5a-d. The anti-HBV activity of selected compounds was studied.