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:
Jan. 07, 2020

Filed:

Jun. 16, 2016
Applicant:

Biocon Limited, Bangalore, IN;

Inventors:

Venkata Raghavendracharyulu Palle, Hyderabad, IN;

Ramakrishna Parameshwar Bhat, Dhareshwar, IN;

Mariappan Kaliappan, Nagamalai, IN;

Jithendra R. Babu, Aragonda, IN;

Rajmahendra Shanmughasamy, Chinnaelasagiri, IN;

Assignee:

BIOCON LIMITED, Bangalore, IN;

Attorney:
Primary Examiner:
Int. Cl.
CPC ...
C07C 255/23 (2006.01); C07C 253/14 (2006.01); C07D 261/08 (2006.01); C07C 253/00 (2006.01); G01N 23/20 (2018.01); G01N 25/48 (2006.01); G01R 33/46 (2006.01);
U.S. Cl.
CPC ...
C07C 255/23 (2013.01); C07C 253/00 (2013.01); C07C 253/14 (2013.01); C07D 261/08 (2013.01); G01N 23/20075 (2013.01); G01N 25/4866 (2013.01); G01R 33/46 (2013.01);
Abstract

The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.


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