7α-(1-HYDROXY-2,2,2-TRIFLUOROETHYL)-17-METHYL-3,6-DIMETHOXY-4,5α-EPOXY-6α,14α-ETHENOISOMORPHINANE AND METHOD FOR PRODUCTION THEREOF Russian patent published in 2014 - IPC C07D489/12 

Abstract RU 2503678 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a novel compound - 7α-(1-hydroxy-2,2,2-trifluoroethyl)-17-methyl-3,6-dimethoxy-4;5α-epoxy-6α,14α-ethenoisomorphinane of formula (1) which is a precursor of fluorine-containing tevinol, tevinols and orvinols, and can be used in production thereof, as well as a method of producing a compound of formula (1) in form of a mixture of (20R)- and (20S)-isomers, which involves reacting an aldehyde of formula with a Ruppert-Prakash reagent [CF3Si(CH3)3], in the presence of a fluoride ion source such as tetrabutylammonium fluoride, in a solvent such as tetrahydrofuran, followed by treatment with and acid and separating the end product using known techniques. Separate (20R)- and (20S)-isomers are separated chromatographically.

EFFECT: improved method.

3 cl, 4 ex

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RU 2 503 678 C1

Authors

Moiseev Sergej Konstantinovich

Kalinin Valerij Nikolaevich

Sandulenko Irina Vladimirovna

Dates

2014-01-10Published

2012-08-21Filed