Preparation method of saxagliptin intermediate

A technology of compound and hydroxyl protecting group, which is applied in the field of preparation of saxagliptin intermediates, can solve the problems of harsh conditions, strong corrosion, and low reaction yield, and achieve low price, mild reaction conditions, and high reaction yield Effect
CN104098481AActive Publication Date: 2014-10-15浙江四维医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
浙江四维医药科技有限公司
Publication Date
2014-10-15

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Abstract

The invention elates to the medicine synthesis field, and concretely relates to a preparation method of a saxagliptin intermediate. A technical scheme adopted in the invention is characterized in that a compound with the structure represented by formula (I) shown in the specification; and in the formula (I), M is hydrogen or various ether hydroxy protection groups, R1 and R2 are H or CH3 respectively independently, and at least one of R1 and R2 is H.
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Description

technical field

[0001] The invention relates to the field of pharmaceutical synthesis, in particular to a preparation method of a saxagliptin intermediate. Background technique

[0002] Saxagliptin, a dipeptidyl peptidase-4 (DPP4) inhibitor, is a drug developed by Bristol-Myers Squibb for the treatment of adult type II diabetes. Its structural formula is as follows:

[0003]

[0004] Saxagliptin

[0005] Under normal circumstances, saxagliptin is subjected to a condensation reaction by the following formula M and formula N compounds, such as the method disclosed in the US patent document US7223573: the condensation product is dehydrated, and the deprotection group is reacted to obtain saxagliptin,

[0006]

[0007] Among them, the main synthetic methods of the compound of formula N structure are as follows:

[0008] Route one:

[0009]

[0010] This route is the method provided in the Chinese patent with the authorization announcement number CN1213028. The SuperH...

Claims

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