Continuous flow teriflunomide preparation process

A technology for teriflunomide and preparation process, which is applied in the field of continuous flow teriflunomide preparation technology, can solve problems such as hazards, and achieve the effects of solving the impact of ring damage, stable process operation, and reducing potential safety hazards.
CN113666842AInactive Publication Date: 2021-11-19河北凯威恒诚制药有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
河北凯威恒诚制药有限公司
Publication Date
2021-11-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a continuous flow teriflunomide preparation process which comprises the following steps: using a continuous flow reactor, taking cyanoacetic acid as a starting material, preparing cyanoacetyl chloride through chlorination, synthesizing a teriflunomide intermediate through the cyanoacetyl chloride and p-trifluoromethylaniline, and synthesizing teriflunomide through the intermediate and acetyl chloride. The method has the advantages of high safety, low cost, low energy consumption and high production yield.
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Description

Technical field

[0001] The present invention relates to the field of chemical synthesis, and more particularly to a process of continuous fluorine amine. Background technique

[0002] Teriflunomide, Chemical Name: (Z) -2-cyano-3-hydroxy-N- [4- (trifluoromethyl) phenyl] -2-butenamide. Tripfluorine is an oral pyrimidine synthase inhibitor and an immunomodulator developed by French Sanopi Avante, which can reverse the inhibitory dihydrochloric acid dehydrogenase (DHODH) - related to the primary synthesis A key enzyme. DHODH is a mitochondrase containing iron-free plain-dependent mitochromese, a critical enzyme in nucleic acid, catalyzed pyrimidine from the fourth step in the head biosynthesis pathway. DHODH is an important target of immune-related diseases, inhibiting DHODH, preventing neonatizine synthesis, causing DNA synthesis disorder, inhibiting activated T lymphocytes, B lymphocytes, and tumor cell proliferation, thereby plays importance in immunosuppression and anti-tumor eff...

Claims

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