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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Authors
Dates
2020-01-27—Published
2018-10-05—Filed