A kind of method of synthesizing thiophene inhibitor TPCA-1

A TPCA-1 and inhibitor technology, applied in the direction of organic chemistry, can solve the problems of cumbersome synthesis steps, harsh conditions, and inconvenient use, and achieve the effects of high yield, mild reaction conditions, and easy-to-obtain reaction raw materials
CN109438416BActive Publication Date: 2020-04-10HENAN NORMAL UNIV
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HENAN NORMAL UNIV
Publication Date
2020-04-10

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Abstract

The invention relates to a method for synthesizing a thiophenes inhibitor TPCA-1, and belongs to the field of organic chemical drug synthesis. The method comprises the following steps: taking thioureaand 2-(4-fluorophenyl) cyclopropane-1,1-dimethyl isophthalate as starting raw materials, and the TPCA-1 is obtained through a multi-step reaction including a ring enlargement reaction, an oxidation reaction, an addition reaction and an amidation reaction in sequence. In the used route of the method, the reaction raw materials are easily obtained, the yield is high, and the TPCA-1 can be obtainedsuccessfully.
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Description

technical field

[0001] The invention relates to a method for synthesizing TPCA-1, which contains thiophene inhibitors, and belongs to the field of organic chemical drug synthesis. Background technique

[0002] TPCA-1 (Chinese name: 5-(4-fluorophenyl)-2-ureidothiophene-3-carboxamide, CAS: 507475-17-4) is a novel and effective selective inhibitor of human IKK-2 . IκB kinase 2 (IKK-2) has been shown to play a key role in nuclear factor κB-regulated production of pro-inflammatory molecules by stimulating tumor necrosis factor-α (TNF-α) and interleukin (IL-1), suggesting that inhibition of IKK- 2 may be beneficial to the treatment of rheumatoid arthritis.

[0003] At present, the synthesis method of this compound is less reported in the literature. For example, in the existing method, it is prepared after five steps of reaction. The reaction equation is as follows:

[0004]

[0005] In the above reaction, the starting material 2,5-dihydroxy-1,4-dithiane has a foul smell, ...

Claims

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