A kind of preparation method of maropitant free base

A technology of free base and reaction formula, which is applied in the field of preparation of raw material drug maropitant free base, can solve the problems of consuming a large amount of solvent and adsorbent, high cost, and long route
CN109320510BActive Publication Date: 2021-04-27WISDOM PHARM CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
WISDOM PHARM CO LTD
Publication Date
2021-04-27

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Abstract

The present invention relates to the preparation method of maropitant free base, and the reaction involves (2S,3R)-2-benzhydrylquinuclidine-3-alcohol and R 1 SO 2 Cl or (CF 3 SO 2 ) 2 O reacts to obtain hydroxyl-protected compound formula IV, and formula IV reacts with 2-methoxy-5-tert-butyl-benzylamine in the presence of a base and a solvent to obtain maropitant free base.
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Description

technical field

[0001] The invention belongs to the technical field of methods for synthesizing raw materials, and in particular relates to the preparation of raw materials Maropitant free base. Background technique

[0002] Maropitant citrate is a type 1 neurokinin (NK1) receptor anti-caking agent that acts on the central nervous system by inhibiting substance P, a key neurotransmitter that causes vomiting. Maropitant citrate is one of the alternative quinine drugs. Due to its remarkable curative effect, the drug was approved by the FDA in 2007 for the prevention and treatment of acute vomiting in dogs, and it was subsequently approved for prescription external use in cats. There are two dosage forms of maropitant citrate, maropitant citrate for injection is used to prevent and treat acute vomiting in dogs; tablet maropitant citrate is used to prevent acute vomiting in dogs and caused by motion sickness vomiting; both are available as a prescription topical drug for cats. ...

Claims

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