1246960-15-5Relevant academic research and scientific papers
Intermediate of Sitagliptin and synthesis method of intermediate
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Paragraph 0090; 0092; 0093; 0094; 0095; 0096; 0097, (2017/07/19)
The invention provides an intermediate of Sitagliptin and a synthesis method of the intermediate. The intermediate is the compound of formula (I), and the synthesis method comprises enabling the compound of the formula (3) to react with cyan-containing salt to obtain the compound of the formula (2), and hydrolyzing the compound of the formula (2) by use of alkali. The synthesis method is short in reaction path, the reaction reagent is cheap, and the expensive reagent in the traditional process is avoided to use, the production cost can be effectively lowered, the synthesis time is shortened, and the industrial production is facilitated. The intermediate of the Sitagliptin manufactured by use of the synthesis method is large in yield, high in purity, and in favor of the preparation of high-quality Sitagliptin.
METHOD FOR PREPARING DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND INTERMEDIATE
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Page/Page column 7, (2012/02/01)
The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor and intermediate. The present invention is able to reduce preparation costs by using low cost reagents on reaction and is able to be used in mass production by improving yield.
METHOD FOR PREPARING SITAGLIPTIN AND AMINE SALT INTERMEDIATES USED THEREIN
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Page/Page column 11, (2011/09/19)
The present invention relates to a method for preparing sitagliptin by using an amine salt of (3R)-3-azido-4-(2,4,5-trifluorophenyl)-butyric acid (formula (V)) in a high yield and purity, and amine salt intermediates used therein.
METHOD FOR PREPARING INTERMEDIATE OF SITAGLIPTIN USING CHIRAL OXIRANE
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Page/Page column 10, (2011/04/25)
Disclosed is: a novel, simple and low-cost method for preparing 3-hydroxy-4-(2,4,5-trifluorophenyl)-butyric acid, particularly (3S)-3-hydroxy-4-(2,4,5-trifluorophenyl)-butyric acid, which is used as a key intermediate in the preparation of sitagliptin.
METHOD OF PREPARING SITAGLIPTIN AND INTERMEDIATES USED THEREIN
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Page/Page column 12, (2011/05/06)
Disclosed are a novel, simple and low-cost method for preparing sitagliptin, as DPP-IV (dipeptidyl peptidase IV) inhibitor, which is useful in treating type 2 diabetes mellitus and key intermediates used in said preparation of sitagliptin.
Process for the synthesis of beta-amino acids and derivatives thereof
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Page/Page column 28, (2012/01/06)
The present invention relates to a process for the preparation of β-amino acids and derivatives thereof, which is especially suited for gliptins and particularly sitagliptin. A key step makes use of suitably derivatized epoxides or aziridines, which owing to a chirality provides a source of chirality for intermediates which are suitable for building up β-amino acids and similar compounds, in particular in the construction of the sitagliptin molecule.
