METHOD OF SYNTHESIS OF 3'-AZIDO-2',3'-DIDEOXYTHYMIDINE Russian patent published in 1999 - IPC

Abstract RU 2135512 C1

FIELD: organic chemistry, chemistry of nucleosides, biochemistry. SUBSTANCE: invention relates to the improved method of synthesis of 3'-azido-2', 3'-dideoxythymidine (azidothymidine) used in medicine as an antiviral preparation for treatment of patients with acquired immunodeficiency syndrome (AIDS). Method involves azidation of 5'-O-benzoyl-2,3'-anhydrothymidine with alkylammonium azides in aprotonic organic solvent (a mixture of dipolar solvent with 1,4-dioxane) followed by isolation of the end substance by the known method. Process is carried out at volume ratio dipolar solvent : 1,4-dioxane = (1.5-1)-(4.0-1) and at 100-110 C. The yield is 85-87%. The use of dipolar solvent in mixture with 1,4-dioxane ensures to increase the yield of the end product and decrease impurity content in it. EFFECT: improved method of synthesis, increased yield and purity. 3 cl, 1 tbl, 1 ex

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Authors

Ostrovskij V.A.(Ru)

Poplavskij V.S.(Ru)

Sherbinin M.B.(Ru)

Malin A.A.(Ru)

Koshtaleva T.M.(Ru)

Khokhrjakova N.R.(Ru)

Bezklubnaja E.V.(Ru)

Kononov A.V.(Ru)

Dates

1999-08-27Published

1997-07-11Filed