METHOD OF PRODUCING (15α,16α,17β)-ESTRA-1,3,5(10)-TRIENE-3,15,16,17-TETROL (ESTETROL) AND INTERMEDIATES IN SAID METHOD Russian patent published in 2024 - IPC C07J1/00 C07J75/00 

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing (15α,16α,17β)-estra-1,3,5(10)-triene-3,15,16,17-tetrol (Estetrol), where said method involves oxidation of (17β)-3-(phenylmethoxy)-estra-1,3,5(10),15-tetraen-17-ol (intermediate 1) to obtain (17β)-3-(phenylmethoxy)-estra-1,3,5(10)-triene-15,16,17-triol (intermediate 2), acetylation of intermediate 2 to obtain (15)α,16α,17β)-3-(phenylmethoxy)-estra-1,3,5(10)-triene-15,16,17-triol triacetate (intermediate 3) through intermediate 3' and conversion of intermediate 3 through (15α,16α,17β)-3-hydroxy-estra-1,3,5(10)-triene-15,16,17-triol triacetate (intermediate 4) into estetrol. Intermediate 3 is converted to intermediate 4 under the following conditions: use of palladium on coal (Pd/C) in amount of 5% or 10% by weight; hydrogen pressure between 1 and 6 bar; linear or branched C_1-6 aliphatic alcohol as a solvent; reaction time of at least 16 hours; hydrogenation temperature between 30 and 60 °C.

EFFECT: production of aestrole on an industrial scale.

9 cl, 5 dwg, 4 tbl, 5 ex