Method of synthesizing apixaban intermediate by microchannel reactor

A microchannel reactor, apixaban technology, applied in organic chemistry and other directions, can solve the problems of low catalyst recovery times, long reaction time, violent explosion, etc., and achieve stable online production and post-processing, yield and purity. The effect of improving and reducing production costs
CN108329314AInactive Publication Date: 2018-07-27HEILONGJIANG XINCHUANG BIOLOGICAL TECH DEV CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HEILONGJIANG XINCHUANG BIOLOGICAL TECH DEV CO LTD
Publication Date
2018-07-27
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method of synthesizing apixaban intermediate by a microchannel reactor and belongs to the technical field of synthesis of antithrombotic drugs. The method comprises: adding ethyl 4,5,6,7-tetrahydro-1-(4-benzyloxyphenyl)-6-(4-nitrophenyl)-7-oxo-1-H-pyrazolo[3,4-c]pyridine-3-carboxylate into an organic solvent, adding an activated carbon-loaded noble metal catalyst to obtain a mixture as material I, delivering the material I to a preheating module of the microchannel reactor, preheating, and feeding into a reaction module unit; delivering hydrogen to the reaction moduleunit of the microchannel reactor and the material I to the reaction module unit for the purpose of reaction, collecting reacted liquid from a cooling module, and post-treating to obtain the apixabanintermediate. The method can effectively shorten the reaction time and greatly reduce the safety potential hazard that hydrogen leakage causes combustion and explosion, and is applicable to the synthesis of apixaban intermediates.
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Description

technical field

[0001] The invention relates to a method for synthesizing an apixaban intermediate in a microchannel reactor, and belongs to the technical field of synthesizing antithrombotic drugs in organic synthesis. Background technique

[0002] Apixaban is an anticoagulant jointly developed by Bristol-Myers Squibb and Pfizer, which can directly act on coagulation factors and is used to treat venous thrombosis diseases including deep vein thrombosis and pulmonary thrombosis. A large number of clinical data at this stage show that oral anticoagulant inhibitors will be widely used to replace traditional intravenous anticoagulants. Because apixaban has good drug safety, low possibility of drug interaction and multiple elimination methods in clinical data, it is expected to be used in special groups of patients with liver disease or renal function impairment, so it has great market prospects .

[0003] The main synthetic method of apixaban is as image 3 As shown, the inte...

Claims

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