Preparation method of teriflunomide and intermediate thereof

A technology for teriflunomide and intermediates, which is applied in the field of preparation of teriflunomide and its intermediates, can solve the problems of corroded equipment, low total yield, cumbersome steps, etc., achieves improved yield, and is conducive to industrial production , the effect of simple operation
CN103848756BActive Publication Date: 2015-04-22HYBIO PHARMA WUHAN CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HYBIO PHARMA WUHAN CO LTD
Publication Date
2015-04-22

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Abstract

The invention belongs to the technical field of medicinal chemistry and discloses a preparation method of teriflunomide and an intermediate thereof. The preparation method of the teriflunomide provided by the invention comprises the following steps: getting a compound with a structure as shown in formula I and an azide in an organic solvent to generate nucleophilic substitution reaction to generate a compound with the structure as shown in formula II; getting and mixing the compound with the structure as shown in the formula II with the organic solvent, heating to obtain the compound with the structure as shown in formula III; under inert-gas protection and alkaline conditions, getting the compound with the structure as shown in the formula III and the compound with the structure as shown in the formula IV to generate electrophilic addition and isomerization reaction in the organic solvent to obtain the teriflunomide. According to the preparation method of the teriflunomide provided by the invention, the reaction intermediate is not needed to be purified, operation is simple, yield of the teriflunomide is improved, production cost of the teriflunomide is lowered, and therefore, the preparation method is more beneficial to industrial production of the teriflunomide.
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Description

technical field

[0001] The invention belongs to the technical field of medicinal chemistry, in particular to a preparation method of teriflunomide and an intermediate thereof. Background technique

[0002] Teriflunomide is an oral pyrimidine synthase inhibitor and immunomodulator, the active metabolite of leflunomide, which blocks the de novo synthesis of pyrimidine by inhibiting dihydroorotate dehydrogenase. Teriflunomide was developed by Sanofi-aventis (Sanofi-Aventis) in the United States and was approved by the FDA on September 12, 2012. Its product name is Aubagio, and it is used for the treatment of relapsing multiple sclerosis. Conduct phase III clinical research. The molecular formula of teriflunomide is: C 12 h 9 f 3 N 2 0 2 , molecular weight is 270.2, has the structure shown in formula V:

[0003]

[0004] As an oral drug, teriflunomide has been approved for the treatment of relapsing-remitting multiple sclerosis in the United States at a dose of 7 mg; i...

Claims

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