7-METHYL-2'-DEOXYGUANOSINE HYDROIODIDE SALT AS SUBSTRATE FOR PRODUCING 2'-DEOXYNUCLEOSIDES BY METHOD OF ENZYME TRANSGLYCOSYLATION Russian patent published in 2018 - IPC C12P19/38 C12N9/10 C12P19/40 

FIELD: biotechnology.

SUBSTANCE: invention relates to the field of biotechnology and pharmaceutical chemistry. Use of the 7-methyl-2'-deoxyguanosine hydroiodide salt to produce 2'-deoxynucleosides by the enzymatic transglycosylation reaction is proposed. 7-methyl-2'-deoxyguanosine hydroiodide salt and base B in the presence of potassium dihydrogen phosphate and E. coli nucleoside phosphorylases are mixed. Base B is , in which R₁=H, F, Cl, NH₂, R₂=NHR or OR, where R=H, methyl, benzyl, phenylethyl and other substituents; or , where R=H, F, methyl, ethyl, isopropyl or other substituents. As nucleic acid phosphorylases, purine nucleoside phosphorylase (PNP) of E. coli and thymidine phosphorylase (TF) of E. coli are used. For the preparation of pyrimidine 2'-deoxyribonucleosides, a mixture of PNP and TF enzymes is used, and to obtain purine 2'-deoxyribonucleosides – PNP enzyme. Hydroiodide salt of 7-Me-dGuo is used in an amount of 1.5 equivalents with respect to base B, and potassium dihydrogen phosphate in an amount of 0.2 to 0.7 equivalents with respect to base B.

EFFECT: invention makes it possible to produce a variety of 2'-deoxyribonucleosides, including therapeutically important nucleosides, and to bring the yields of the target nucleosides to substantially quantitative by HPLC and at least 80 % after isolation and chromatographic purification.

1 cl, 4 dwg, 1 tbl, 7 ex