Sitagliptin synthesis method

A synthetic method and step-by-step technology, applied in the field of medicine and chemical industry, can solve the problems of resource waste, many steps, expensive raw materials, etc., and achieve the effects of avoiding toxic and dangerous chemical reagents, mild reaction conditions, and easy-to-obtain raw materials
CN108178761AInactive Publication Date: 2018-06-19安庆奇创药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
安庆奇创药业有限公司
Publication Date
2018-06-19
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a sitagliptin synthesis method, which comprises: carrying out a reaction on a compound represented by a formula IV, (R)-(+)-tert-butyl sulfinamide and hydrogen under the catalysis of a catalyst to obtain a compound represented by a formula V; and carrying out a hydrolysis reaction on the compound represented by the formula V to obtain a compound represented by a formula VI,ie., sitagliptin. According to the present invention, the method has advantages of easily available raw materials, simple steps, high yield and mild reaction conditions, and is suitable for industrial production. The formulas IV, V and VI are defined in the specification.
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Description

technical field

[0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a synthesis method of sitagliptin. Background technique

[0002] The chemical name of sitagliptin is 7-[(3R)-3amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetra Hydrogen-3-trifluoromethyl-1,2,4-triazolo[4,3-a]pyrazine is an oral DPP-IV inhibitor for the treatment of type II diabetes. Sitagliptin was approved for marketing in 2006 and is the best-selling variety. In 2015, the total sales of Januvia and Janumet reached US$6.29 billion, making it the largest variety among DPP-IV inhibitors.

[0003] Initially, Merck applied for the patent CN1761642 for the preparation method of the compound, which disclosed that 2,4,5-trifluorophenylacetic acid was used as the starting material, and first reacted with cyclo(ethylene)isopropyl malonate to form The corresponding enol compound is followed by substitution and decarboxylation with the corresponding pyraz...

Claims

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