FIELD: pharmaceuticals.
SUBSTANCE: invention relates to a method of producing a fenfluramine active pharmaceutical ingredient. Disclosed method includes steps (a)—(e). Step (a) comprises hydrolysis of 2-(3-(trifluoromethyl)phenyl)acetonitrile composition to obtain composition of 2-(3-(trifluoromethyl)phenyl)acetic acid. At step (b), composition of 2-(3-(trifluoromethyl)phenyl)acetic acid is purified to obtain purified composition 2-(3-(trifluoromethyl)phenyl)acetic acid. At step (c), purified 2-(3-(trifluoromethyl)phenyl)acetic acid composition is reacted with acetic anhydride and a catalyst to obtain composition of 1-(3-(trifluoromethyl)phenyl)propan-2-one. Composition (d) comprises purifying composition 1-(3-(trifluoromethyl)phenyl)propan-2-one using a ketone bisulphite adduct to obtain a purified composition of 1-(3-(trifluoromethyl)phenyl)propan-2-one. Composition (e) comprises reductive amination of 1-(3-(trifluoromethyl)phenyl)propan-2-one with ethylamine using a borohydride reducing agent to obtain a crude fenfluramine composition containing trifluoromethyl-phenyl regioisomers of fenfluramine or salts thereof in a total amount of less than 0.2 wt %.
EFFECT: disclosed method enables to obtain a fenfluramine active pharmaceutical ingredient from which certain undesirable secondary components are removed.
21 cl, 10 tbl, 5 ex, 5 dwg
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