ENZYMATIC SYNTHESIS OF 4'-ETHYNYL NUCLEOSIDE ANALOGUES Russian patent published in 2024 - IPC C07C29/00 C07C33/42 C07F9/113 A61K31/496 A61K31/7068 C12P19/40 C07H1/00 

Abstract RU 2816846 C2

FIELD: chemistry.

SUBSTANCE: invention relates to a method for synthesis of 4'-ethynyl-2'-deoxynucleoside, comprising combining compound 6.5

with purine nucleoside phosphorylase and a nucleobase in a buffer solution containing a manganese (II) salt, where 2X+ is (a) two protons, (b) one proton and one monovalent cation, (c) two monovalent cations, where each cation is the same or they are different from each other, or (d) one divalent cation, and where 4'-ethynyl-2'-deoxynucleoside is

.

Invention also relates to novel intermediate compounds and methods for production thereof.

EFFECT: novel method of producing 4'-ethynyl-2'-deoxynucleoside, which eliminates the use of protective groups on intermediate compounds, improves stereoselectivity of glycosylation and reduces the number of process steps.

32 cl, 3 tbl

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RU 2 816 846 C2

Authors

Khaffmen, Mark, A.

Friszkovska, Anna

Kolev, Dzhoshua, N.

Devajn, Pol, N.

Kampos, Kevin, R.

Trappo, Mettyu

Navrat, Kristofer, S.

Dates

2024-04-05Published

2019-07-02Filed