CHIRAL REAGENTS FOR PRODUCTION OF HOMOGENOUS OLIGOMERS Russian patent published in 2023 - IPC C07F9/6558 C07F9/6561 C07H21/00 

FIELD: chemistry.

SUBSTANCE: present invention relates to a method for the production of essentially diastereomeric pure phosphorodiamidate morpholino-oligomer containing chiral phosphoric bonds, which is used for the production of stereo-chemically pure oligonucleotide. The proposed method includes following stages: selection of essentially stereo-chemically pure phosphoramidochloride morpholino-monomers; and synthesis of essentially diastereomeric pure phosphorodiamidate morpholino-oligomer by stereo-specific combination of selected essentially stereo-chemically pure phosphoramidochloride morpholino-monomers, where the specified stereo-specific combination is carried out in an aprotic solvent in the presence of non-nucleophilic tertiary amine or aromatic base, at a temperature from 20°C to 50°C. At the same time, essentially stereo-chemically pure phosphoramidochloride morpholino-monomers are obtained by separation of a diastereomeric mixture of phosphoramidochloride morpholino-monomers into essentially stereo-chemically pure phosphoramidochloride morpholino-monomers. Essentially stereo-chemically pure, in this case, relates to enantiomers or diastereomers, which are in enantiomeric or diastereomeric excess, respectively, equal to or more than 87%, and essentially diastereomeric pure relates to diastereomers, which are in diastereomeric excess equal to or more than 87%.

EFFECT: obtainment of a method for the production of oligomers.

6 cl, 11 dwg, 2 tbl, 4 ex