- BOC-(R)-3-amino-4-(2,4,5-trifluorophenyl)butyric acid condensation impurity and preparation method thereof
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The invention provides a sitagliptin phosphate important intermediate BOC-(R)-3-amino-4-(2,4,5-trifluorophenyl)butyric acid condensation impurity and a preparation method and preparation thereof. TheBOC-(R)-3-amino-4-(2,4,5-trifluorophenyl)butyric acid condensation impurity and the preparation method thereof have important significance for the following industrial production of bulk drugs.
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- A phosphoric acid west geleg sandbank crystal and its preparation and use
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The invention provides a crystal-type sitagliptin phosphate monohydrate and a preparation method, pharmaceutical composition and application thereof. The solubility of the sitagliptin phosphate crystal is high and obviously higher than that of a sitagliptin phosphate monohydrate in the prior art, and the sitagliptin phosphate crystal is good in both stability and hygroscopicity under the conditions of high temperature, high humidity and illumination. Compared with the prior art, the crystal-type sitagliptin phosphate monohydrate has the advantages that the solubility is higher, and the great significance for improving the pharmaceutical effect and reducing the pharmaceutical loading capacity is achieved; the preparation method is easy to operate, good in repeatability and beneficial for cost control in industrialized production and has the extremely high economic value; the time period of industrialized mass production is greatly shortened, the production efficiency is improved, the production energy consumption is reduced, and the cost of industrialized mass production is lowered.
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Paragraph 0070; 0077; 0080; 0083; 0086; 0089; 0092; 0095
(2018/11/03)
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- Practical and economical approach to synthesize sitagliptin
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Economic syntheses of sitagliptin phosphate monohydrate, acknowledged as the first dipeptidyl peptidase 4 (DPP-4) inhibitor, have been achieved in an overall yield of 42.4% in four steps from 1-{3-(trifluoromethyl)-5,6-dihydro-[1, 2,4]triazolo[4,3-a]pyrazin-7(8H)-yl}-4-(2,4,5-trifluorophenyl)butane-1,3-dione. The key stereoselective reduction of this process was carried out by NaBH 4/HCOOH instead of expensive and toxic catalysts or ligands. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications for the following free supplemental resource(s): Full experimental and spectral details.]
- Lin, Kuaile,Cai, Zhengyan,Zhou, Weicheng
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p. 3281 - 3286
(2013/10/01)
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- SITAGLIPTIN, SALTS AND POLYMORPHS THEREOF
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The present invention relates to an improved process for preparation of Sitagliptin or pharmaceutically acceptable salts thereof. The present invention further relates to novel polymorphs of Sitagliptin salts and process for preparation thereof.
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Paragraph 0204
(2013/06/28)
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- AMORPHOUS FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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The present invention relates to a novel amorphous form of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-a mine as well as a process for its preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.
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Page/Page column 14
(2008/06/13)
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- NOVEL CRYSTALLINE FORM OF A PHOSPHORIC ACID SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR
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The present invention relates to a novel crystalline anhydrate polymorph of the dihydrogenphosphate salt of (2R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-a mine as well as a process for their preparation, pharmaceutical compositions containing this novel form, and methods of use of the novel form and pharmaceutical compositions for the treatment of diabetes, obesity, and high blood pressure.
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