401566-80-1Relevant articles and documents
AN IMPROVED PROCESS FOR THE PREPARATION OF TENELIGLIPTIN HYDROBROMIDE HYDRATE
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Page/Page column 7-8, (2021/01/23)
The present invention provides an improved process for the preparation of Teneligliptin HBr more particularly relates to a process for the preparation of Teneligliptin 2.5HBr hydrate salt.
Method for preparing hydrobromic acid teneligliptin
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, (2017/07/01)
The invention provides a method for preparing hydrobromic acid teneligliptin. The method includes steps of preparing L-hydroxyproline; mixing the L-hydroxyproline and sodium bicarbonate with each other to obtain mixtures, dissolving the mixtures in water, adding acetone into the water, dropping di-tert-butyl dicarbonate into the water, carrying out room-temperature reaction overnight and then treating reaction products to obtain t-butyloxycarboryl-N-hydroxyproline; preparing t-butyloxycarboryl-N-4-oxo-proline from the t-butyloxycarboryl-N-hydroxyproline; preparing (2S)-4-oxo-2-(3-thiazolidine carbonyl)-1-pyrrolidine carboxylic acid tert-butyl ester from the t-butyloxycarboryl-N-4-oxo-proline; preparing compounds III from compounds IV; preparing compounds II from the compounds III; preparing compounds 1-(3-methyl-1-phenyl-1H-pyrazole-5-base) piperazine from the compounds II; preparing intermediates I; preparing the hydrobromic acid teneligliptin from the intermediates I. The method has the advantages that the method is low in cost, and the cost of the method is only two-thirds of the cost of an existing method in the prior art; the yield of the hydrobromic acid teneligliptin is higher than 95%, and the purity of the hydrobromic acid teneligliptin is higher than 98%.
PROCESS FOR THE PREPARATION OF 1-(3-METHYL-1-PHENYL-1H-PYRAZOL-5-YL)PIPERAZINE
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Page/Page column 8; 9, (2015/05/19)
The present invention provides a process for the preparation of 1-(3-methyl-1- phenyl-1H-pyrazol-5-yl)piperazine of Formula III, or salts thereof. The invention also provides a process for the preparation of {(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-