Invention Grant
- Patent Title: Process for the preparation of teriflunomide
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Application No.: US15736981Application Date: 2016-06-16
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Publication No.: US10526279B2Publication Date: 2020-01-07
- Inventor: Venkata Raghavendracharyulu Palle , Ramakrishna Parameshwar Bhat , Mariappan Kaliappan , Jithendra R. Babu , Rajmahendra Shanmughasamy
- Applicant: BIOCON LIMITED
- Applicant Address: IN Bangalore
- Assignee: BIOCON LIMITED
- Current Assignee: BIOCON LIMITED
- Current Assignee Address: IN Bangalore
- Agency: Katten Muchin Rosenman LLP
- Priority: IN3028/CHE/2015 20150617
- International Application: PCT/IB2016/053556 WO 20160616
- International Announcement: WO2016/203410 WO 20161222
- Main IPC: C07C255/23
- IPC: C07C255/23 ; C07C253/14 ; C07D261/08 ; C07C253/00 ; G01N23/20 ; G01N25/48 ; G01R33/46

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.
Public/Granted literature
- US20180170859A1 A NOVEL PROCESS FOR THE PREPARATION OF TERIFLUNOMIDE Public/Granted day:2018-06-21
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