1246610-74-1Relevant articles and documents
Preparation method of alogliptin benzoate
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, (2021/01/29)
The invention discloses a preparation method of alogliptin benzoate. Main starting materials of the preparation method are 6-chloro-3-methyluracil, o-cyanobenzyl bromide, (R)-3-Boc-aminopiperidine andbenzoic acid. According to the method, all indexes meet the specification, meanwhile, dangerous reagents such as sodium hydride and highly toxic methyl iodide are prevented from being used in the reaction process, the requirement for the operation process is not strict, and water-free and oxygen-free conditions are not needed; a high-boiling-point mixed solvent is not used in the reaction, and the solvent is easy to recycle; the selected starting materials are available in the market and easy to obtain, and large-scale production is facilitated; in addition, starting materials or intermediates in the synthetic route are good in stability and convenient to store and control, and genotoxic impurities are avoided in the reaction process; and the synthesis process is environment-friendly.
A synthetic [...] intermediates
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, (2019/06/05)
The present invention provides a method for synthesizing an intermediate V. The method comprises: (a) allowing a compound I and a compound II to react while being heated in a solvent under an alkaline condition to obtain an intermediate III; and (b) the intermediate III reacting with a compound IV in the solvent under the alkaline condition to obtain the intermediate V. The intermediate V can be used to synthesize alogliptin.
Preparation and after-treatment method for high-purity alogliptin benzoate
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, (2017/08/29)
The invention relates to optimization and improvement of a preparation and after-treatment method for alogliptin benzoate. In the Boc deprotection process, alkali extraction and acid precipitation methods are adopted, and impurities which do not contain basic groups are effectively removed on the basis of simplifying the process. Moreover, the solvent and temperature control is optimized in the salifying process, and the product quality and yield are improved.