The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.

The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.

Date of Patent:
Mar. 16, 2021

Filed:

Jun. 04, 2019
Applicant:

Zogenix International Limited, Berkshire, GB;

Inventors:

Derek J. Londesbrough, Sunderland, GB;

Marc W. Andersen, Raleigh, NC (US);

Assignee:
Attorneys:
Primary Examiner:
Int. Cl.
CPC ...
C07C 209/28 (2006.01); C07C 51/43 (2006.01); C07C 51/08 (2006.01); C07C 45/80 (2006.01); C07C 45/72 (2006.01); C07C 209/84 (2006.01);
U.S. Cl.
CPC ...
C07C 209/28 (2013.01); C07C 45/72 (2013.01); C07C 45/80 (2013.01); C07C 51/08 (2013.01); C07C 51/43 (2013.01); C07C 209/84 (2013.01); C07B 2200/13 (2013.01);
Abstract

Methods of preparing a fenfluramine active pharmaceutical ingredient are provided. Aspects of the method include (a) hydrolyzing a 2-(3-(trifluoromethyl)phenyl)acetonitrile composition to produce a 2-(3-(trifluoromethyl)phenyl)acetic acid composition; (b) reacting the 2-(3-(trifluoromethyl)phenyl)acetic acid composition with acetic anhydride and a catalyst to produce a 1-(3-(trifluoromethyl)phenyl)propan-2-one composition; and (c) reductively aminating the 1-(3-(trifluoromethyl)phenyl)propan-2-one composition with ethylamine using a borohydride reducing agent to produce a fenfluramine composition. Also provided are compositions and pharmaceutical ingredients prepared according to the subject methods including a pharmaceutically acceptable salt of fenfluramine and having less than 0.2% by weight in total of trifluoromethyl regioisomers.


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