The preparation method of the key intermediate 1 for the synthesis of baricitinib

A technology of baricitinib and intermediates, which is applied in the field of preparation of key intermediate 1, can solve the problems of high cost and cumbersome operation, and achieve the effects of low cost, simple purification and mild reaction conditions
CN107739328BActive Publication Date: 2020-03-20海化生命(厦门)科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
海化生命(厦门)科技有限公司
Publication Date
2020-03-20

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Abstract

The invention relates to a preparation method for synthesizing a key intermediate 1 of Baricitinib. The preparation method comprises the following steps: generating ring closing reaction by virtue of1,3-dibromo-2,2-dimethoxypropane (SM) and ethyl sulfonamide (SM2) under an alkaline condition, and carrying out acetal deprotection under an acidic condition, so as to obtain an intermediate B; and generating witting reaction by virtue of the obtained intermediate B and diethyl cyanomethylphosphonate under the alkaline condition, so as to obtain the key intermediate 1. According to the preparationmethod, the ring closing reaction is generated by virtue of the commercial materials SM and ethyl sulfonamide under the alkaline condition, acetal deprotection is carried out under the acidic condition so as to obtain intermediate B, and witting reaction is carried out so as to obtain the key intermediate 1; the key intermediate 1 can be actually obtained only through two synthetic steps; and compared with the prior art, the preparation method has the advantages that the synthetic route is greatly shortened, the hydrogenation is avoided, and the production cost of the key intermediate 1 is lowered.
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Description

technical field

[0001] The present invention relates to a preparation method for the key intermediate 1 used in the synthesis of baricitinib. Background technique

[0002] Rheumatoid arthritis (RA) is an autoimmune disease characterized by joint inflammation and progressive destruction of joints. There are more than 23 million RA patients worldwide, and the disease affects about three times as many women as men. Both patients and physicians say there are still significant opportunities to improve patient care. Current RA treatment includes the use of non-steroidal anti-inflammatory drugs, oral disease-modifying drugs such as methotrexate, and injectable biologics that selectively target biotransmitters involved in the pathogenesis of RA, such as adalimumab. However, because the price of biological agents is quite expensive, it is only suitable for a small number of groups, so oral chemical drugs are the mainstream drugs for the treatment of RA.

[0003] Baricitinib is a s...

Claims

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