Sitagliptin impurity synthesis method

A sitagliptin impurity and synthesis method technology, applied in the field of sitagliptin impurity synthesis, can solve the problems of long route, complex reaction, low yield, etc.
CN105085531AActive Publication Date: 2015-11-25HEFEI HUAFANG PHARMA SCI & TECH
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HEFEI HUAFANG PHARMA SCI & TECH
Publication Date
2015-11-25

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Abstract

The invention discloses a sitagliptin impurity synthesis method. According to the method, sitagliptin is taken as a raw material, and a sitagliptin impurity is obtained through a deamination reaction under an acidic or alkali condition. The purity of the sitagliptin impurity obtained according to the method can reach 99% or higher, and thus the sitagliptin impurity can serve as a reference substance for quality research.
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Description

[0001] Field of the invention: the present invention relates to the field of organic chemistry, which is the elimination reaction of amino groups, specifically a method for synthesizing sitagliptin impurities. Background technique

[0002] Sitagliptin was developed and marketed by Merck as the first dipeptidyl peptidase-4 (DPP-4) inhibitor. The drug was launched in the United States on October 16, 2006 and March 30, 2007 , the drug was approved by the US FDA in combination with metformin for the treatment of type 2 diabetes, and the drug has been marketed in many European countries. In August 2009, the drug was approved by the European Union as a first-line drug for the treatment of type 2 diabetes. In December 2009, Ono launched sitagliptin in Japan for the treatment of type 2 diabetes. In May 2011, Japan approved the drug in combination with alpha glucosidase inhibitors. In September 2011, Japan approved the drug Combination medication with insulin.

[0003] The chemical n...

Claims

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