FIELD: chemistry.
SUBSTANCE: invention relates to a method of producing a compound of formula (III) by selective acylation of rapamycin in 42 position using an acylation reagent of formula (I), in which R4 and R5 denote residue ketal residue of formula II, in presence of a base, which is pyridine, optionally in presence of an additional solvent S, as well as a method for synthesis of temsirolimus, involving synthesis of formula (III) according to present invention.
EFFECT: technical result is obtaining a compound of formula (III) with high output and regioselectivity, low cost and number of equivalents of reagents.
10 cl, 1 tbl, 3 ex
| Title | Year | Author | Number |
|---|---|---|---|
| RAPAMYCIN HYDROXYESTERS, METHOD OF THEIR SYNTHESIS AND METHODS OF TREATMENT | 1995 |
|
RU2134267C1 |
| C-22 STABILIZED DERIVATIVES OF RAPAMYCIN, METHOD OF IMMUNO- -SUPPRESSION INDUCING, METHOD OF TREATMENT AND PROPHYLAXIS OF TRANSPLANT REJECTION OR HOMOLOGOUS DISEASE, METHOD OF TREATMENT OR PROPHYLAXIS OF HYPERPROLIFERATIVE VASCULAR DISORDER | 1994 |
|
RU2152946C1 |
| TETRAHYDROQUINOLIN DERIVATIVES, BASED PHARMACEUTICAL COMPOSITION BASED ON THEM AND THEIR APPLICATION AS FERTILITY MODULATOR | 2003 |
|
RU2328488C2 |
| IMIDAZO[4,5-C]PYRIDINE DERIVATIVES AS TOLL-LIKE RECEPTOR AGONISTS | 2020 |
|
RU2785124C1 |
| METHODS FOR EPLERENONE OBTAINMENT | 2003 |
|
RU2339642C9 |
| REGIOSPECIFIC SYNTHESIS OF RAPAMYCIN 42-ESTER DERIVATIVES | 2005 |
|
RU2387657C2 |
| BICYCLIC N-ACYLATED IMIDAZO-3-AMINE OR IMIDAZO-5-AMINE SALTS, METHOD FOR THEIR PREPARING AND PHARMACEUTICAL COMPOSITION BASED ON THEREOF | 2001 |
|
RU2268888C2 |
| STILBENOID COMPOUNDS AS INHIBITORS OF SQUAMOUS CELL CARCINOMA AND HEPATOMA AND USE THEREOF | 2014 |
|
RU2594281C2 |
| 1,4 THIAZEPINES/SULPHONES AS BACE1 AND/OR BACE2 INHIBITORS | 2012 |
|
RU2600931C2 |
| 3-SUBSTITUTED DERIVATIVES OF 3H-2,3-BENZODIAZEPINE, METHOD OF THEIR SYNTHESIS AND PHARMACEUTICAL COMPOSITION | 1995 |
|
RU2146678C1 |
