Synthetic process of anti-hyperglycemic drug intermediate R-3-amino-piperidine dihydrochloride

An anti-hyperglycemia, R-3- technology, applied in the production of bulk chemicals, organic chemistry, etc., can solve the problems of low total yield and limited application, and achieve high total yield, cheap raw materials, and atom economy Good results
CN110372573AInactive Publication Date: 2019-10-25苏州汉德创宏生化科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
苏州汉德创宏生化科技有限公司
Publication Date
2019-10-25
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a synthetic process of an anti-hyperglycemic drug intermediate R-3-amino-piperidine dihydrochloride. The synthetic process comprises the steps: using inexpensive L-glutamic acid as a starting material, and performing esterification, amino protection, reduction, hydroxyl protection, substitution, cyclization and removal of protecting groups for amino groups so as to obtainthe R-3-amino-piperidine dihydrochloride. Compared with the prior art, the synthetic process has cheap and easily available raw materials, good selectivity, good atomic economy, high total yield and mild reaction conditions, and is suitable for industrial production.
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Description

technical field

[0001] The invention relates to the field of pharmaceutical intermediates, in particular to a synthesis process of R-3-amino-piperidine dihydrochloride, an antihyperglycemic pharmaceutical intermediate. Background technique

[0002] R-3-amino-piperidine dihydrochloride is an important drug intermediate, and the synthesis of linagliptin, alogliptin, linagliptin, etc. requires the use of R-3-amino-piperidine dihydrochloride Hydrochloride is used as an intermediate, so the synthesis of this compound is widely used in the field of medicine.

[0003] The traditional methods of synthesizing R-3-amino-piperidine dihydrochloride have obvious shortcomings. For example, the reduction reaction of some relatively complex precursor molecules containing R-3-amino-piperidine framework is carried out to obtain R-3-amino-piperidine dihydrochloride, and the reaction in the conversion requires relatively high temperature and oxidant, or The use of highly toxic pyridine deriva...

Claims

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