The invention discloses d4T-5'-hydro-ortho-
phosphorous acid menthol ester and a preparation method and application thereof, relates to
nucleoside hydro-ortho-
phosphorous acid ester and provides d4T-5'-hydro-ortho-
phosphorous acid menthol ester and a preparation method and application thereof. The d4T-5'-hydro-ortho-phosphorous acid
menthol ester is a white
solid and has the chemical name being 2',3'-bisdehydro-2',3'bideoxythymidine-5'-hydro-ortho-phosphorous acid menthol ester, the molecular formula being C20H32N2O6P, and the relative molecular
mass being 426. The preparation method comprises the following steps of: condensing d4T and menthol with two hydroxyl groups of ortho-phosphorous acid in sequence in a basic
solvent by taking pivaloyl
chlorine as a condensing agent; and synthesizing d4T-5'-hydro-ortho-phosphorous acid menthol ester in a one-kettle way. The prepared d4T-5'-hydro-ortho-phosphorous acid menthol ester can restrain the activity of
reverse transcriptase, is taken as an inhibitor of
nucleoside reversed transcriptive
enzyme, and is widely applied to the preparation of an anti-acquired
immune deficiency syndrome medicament. The method has the advantages of readily available synthesis raw materials, short reaction time, less steps, mild condition and yield up to 69 percent.