Synthesis method of fosaprepitant dimeglumine

A synthesis method and technology for fosaprepitant, applied in the field of medicine, can solve the problems of inconvenient preparation method, the yield needs to be improved, etc., and achieve the effects of saving steps and solvents, avoiding secondary pollution, and saving steps
CN111662329AActive Publication Date: 2020-09-15LIANYUNGANG GUIKE PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
LIANYUNGANG GUIKE PHARMA
Publication Date
2020-09-15

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Abstract

The invention discloses a synthesis method of fosaprepitant dimeglumine, and belongs to the technical field of medicines. The synthesis method of fosaprepitant dimeglumine mainly comprises the following steps: reacting tetrabenzyl pyrophosphate, adsorbing impurity tar, hydrogenating palladium mesoporous carbon, refining and the like. According to the invention, a one-pot reaction is adopted; a dibenzyl ester product is generated; sodium carbonate is added for quenching reaction, mesoporous carbon is added for adsorbing impurities and tar, palladium-carbon catalyst deactivation is avoided, thena tetrahydrofuran system is directly utilized for a reaction, palladium mesoporous carbon has high activity and can generate monobenzyl ester first and then remove groups through hydrogenation compared with a common route, steps are saved, and high yield is achieved.
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Description

technical field

[0001] The invention belongs to the technical field of medicine, in particular to a method for synthesizing fosaprepitant dipglumine. Background technique

[0002] Fosaprepitant Diglumine is a water-soluble phosphoryl prodrug of Aprepitant. After intravenous injection, it can be quickly converted into Aprepitant through phosphorylation in the body. It is suitable for patients who cannot be taken orally, Patients with difficulty swallowing or poor digestion. Fosaprepitant dimglumine and aprepitant belong to a group of selective high-affinity receptor blockers called human substance P / neurokinin 1 (NK-1), which mainly block nausea and vomiting signals in the brain mechanism of action.

[0003] At present, most of the synthesis methods of fosaprepitant dimeglumine reported in the literature are palladium-catalyzed hydrogenation in the last step, which requires high-pressure reactors, has poor safety, and the production scale is severely limited, so it is not s...

Claims

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