IMPROVED METHOD OF PRODUCING NALMEFENE FROM NALTREXONE Russian patent published in 2020 - IPC C07D489/08 

Abstract RU 2712232 C1

FIELD: chemistry.

SUBSTANCE: invention relates to a method of producing nalmefene hydrochloride (17-(cyclopropylmethyl)-4,5-alpha-epoxy-6-methylenimorphinan-3,14-diol hydrochloride) from naltrexone (17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroximiminan-6-one) by Wittig reaction, characterized by that when forming phosphorus ylide and in a subsequent reaction of ylide with naltrexone, a reagent is used in which extremely soluble naltrexone and well soluble nalmefene is used, and it is tert-butyl methyl ether (2-methyl-2-methoxypropane, MTBE).

EFFECT: technical result is an improved method which enables efficient and selective process of producing nalmefene by Wittig reaction on an industrial scale with high output of the end product and high degree of purity.

21 cl, 2 dwg, 1 tbl, 5 ex

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RU 2 712 232 C1

Authors

Kuznetsov Viktor Anatolevich

Krivorotov Denis Viktorovich

Shchipalkin Andrej Aleksandrovich

Abzianidze Viktoriya Vadimovna

Martinovich Nikolaj Nikolaevich

Radilov Andrej Stanislavovich

Rembovskij Vladimir Romanovich

Dulov Sergej Anatolevich

Kiselev Dmitrij Borisovich

Erofeev Gennadij Grigorevich

Dates

2020-01-27Published

2018-10-05Filed