CHEMICAL COMPOUND WITH A TRIAZINE GROUP AND A METHOD OF ITS PREPARATION Russian patent published in 2023 - IPC C07H21/00 A61K31/712 

FIELD: pharmaceuticals.

SUBSTANCE: invention relates to a compound corresponding to the formula F0, in which the substituent Z is selected from the following group: -OH, -SH, -SeH, -NHR^N, -O-PG, -S-PG, -Se-PG or -N(PG)R^N; X and Y substituents are selected from the group consisting of the 5'-O-terminus of the nucleoside or oligonucleotide, the 3'-O-terminus of the nucleoside or oligonucleotide, –H, –OH, –SH, –NHR^N, –O-PG or – S-PG, monophosphate, diphosphate, linker; wherein either X or Y is the 5'-O-terminus of the nucleoside or oligonucleotide or the 3'-O-terminus of the nucleoside or oligonucleotide; substituents R¹, R², R³, R⁴ are selected from the range -H, -C_1-18 alkyl, -C_2-18 alkenyl, -C_2-18 alkynyl and -C_6-18aryl, which may include groups –NH–, –N<, –O–, –NHC(O)–, –NHS(O)₂ –, –N(CH₂CH₂)₂N– and/or structures (a) bonded to two atoms carbon of the main chain of the substituent, and also end with the groups –NR ₂, –OR, –SR, –OC(O)R, –NHC(O)R, –C(O)OR, –C(O)NHR, –N= C(N(R₂)₂, –S(O)R, –S(O)₂ R, –S(O)₂NR₂, –CN, –Cl, –Br, –I, –F, –N₃, (c) or (c); while PG is a protective group, chemically inert during automatic synthesis, cleaved off at the stage of the final deblocking of oligonucleotides, while R^N is –H or –C_1-4 alkyl; the pairs R1 and R2, R3 and R4, R5 and R6, R7 and R8 together with their associated nitrogen atom optionally form a 5–8 membered heterocyclic substituent selected from N-pyrrolidinyl, N-piperidinyl, N-azepanyl, N-azocanyl or N-piperazinyl. The invention relates to processes for the preparation of compounds according to the invention of the formula F0. The production method is carried out by reacting a trivalent phosphorus derivative of the formula (F1) with an azidotriazine of the formula (F2), followed by obtaining a compound of the formula (F0). The production method is also carried out by reacting a trivalent phosphorus derivative of formula (F1) with an azidotriazine of formula (F3) to obtain a compound of formula (F4) followed by transformations into a compound of formula (F0).

EFFECT: compounds for use as a research tool, in vitro and in vivo, acting through the formation of a complementary complex with the target nucleic acid.

17 cl, 10 dwg, 1 tbl, 49 ex