ASYMMETRIC AUXILIARY GROUP Russian patent published in 2019 - IPC C07D207/08 C07B53/00 C07F7/10 C07H21/04 C07H23/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a chiral reagent of formula (I') to obtain nucleoside derivative 3'-phosphoramidite of formulas (Va') or (Vb'), which can be used in chemical industry for synthesis of oligonucleotides: (I'), where G¹ is H or a group of formula (II), G² represents a group of formulas (III) or (V), or G¹ and G² together form a group of formula (IV), (II), (III), (IV), (V), where G²¹–G²³ are H or a nitro group, G³¹–G³³ are represented by C_1-4 alkyl or C_6-14 aryl, G⁴¹–G⁴⁶ are H, G⁵¹–G⁵³ are H or C_1-3 alkyl. Disclosed are new reagents and nucleoside derivatives obtained using them 3'-phosphoramidite of formulas (Va') or (Vb'), effective for oligonucleotide synthesis, (Va’), (Vb’), where G⁵ is 4,4'-dimethoxytrityl, R² is H, O-C_1-6alkyl, halogen, R³ is-CH₂-, and Bs is selected from residues of unmodified and modified nucleosides. Disclosed are novel efficient methods of synthesis of said oligonucleotide derivatives.

EFFECT: asymmetric auxiliary group is proposed.

14 cl, 69 ex, 1 tbl, 2 dwg