- A sand geleg sandbank salt and its preparation method
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The invention relates to a saxagliptin salt and a preparation method thereof. The saxagliptin salt has a structure represented by the formula II. Saxagliptin p-toluene sulfonate with a stable crystal form can be obtained through the salt-forming reactions between saxagliptin free alkali and p-toluene sulfonic acid under different solution systems. Stability researches show that saxagliptin p-toluene sulfonate has a better thermal stability than that of saxagliptin monohydrate and saxagliptin hydrochloride. Moreover, the preparation method of the saxagliptin salt is simple and is suitable for industrial production.
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Paragraph 0036; 0037
(2018/11/03)
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- PROCESS FOR PREPARING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREFOR
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A process for preparing an amine of the structure which comprises a. treating an aqueous solution of a keto acid of the structure with ammonium formate, nicotinamide adenine dinucleotide, dithiothreitol and partially purified phenylalanine dehydrogenase and/or formate dehydrogenase enzyme (PDH/FDH); and b. adjusting pH of the reaction mixture with sodium hydroxide to form the desired amine which is substantially free of undesirable excess ammonium ions.
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- A PROCESS FOR PREPARATION OF SAXAGLIPTIN AND ITS HYDROCHLORIDE SALT
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Described is an improved and industrially feasible process for the preparation of Saxagliptin or its hydrochloride salt. Also described are the novel intermediates and their use in the preparation of Saxagliptin or its hydrochloride salt.
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- PROCESS FOR PREPARATION OF (IS, 3S, 5S)-2-[(2S)-2-AMIN0-2-(3-HYDROXY-l-ADAMANTYL) ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE
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Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
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- SAXAGLIPTIN HYDROCHLORIDE SOLID DISPERSION
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The present invention provides a novel amorphous solid dispersion of saxagliptin hydrochloride in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
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Page/Page column 7
(2014/07/21)
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- PROCESS FOR PREPARATION OF (1S, 3S, 5S)-2-[(2S)-2-AMINO-2-(3-HYDROXY-1-ADAMANTYL) ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE
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Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin.
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- PROCESS FOR THE PREPARATION OF (1S, 3S, 5S)-2-[2(S)-2-AMINO-2-(3-HYDROXY-1-ADAMANTAN-1-YL ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE
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The present invention relates to an improved process for the preparation of (1S,3S,5S)-242(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its intermediates.
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- POLYMORPHS OF SAXAGLIPTIN HYDROCHLORIDE AND PROCESSES FOR PREPARING THEM
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The invention provides polymorphs of Saxagliptin hydrochloride, processes for preparing polymorphs of Saxagliptin hydrochloride, and pharmaceutical compositions of polymorphs of Saxagliptin hydrochloride.
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Page/Page column 6
(2012/04/11)
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- SAXAGLIPTIN INTERMEDIATES, SAXAGLIPTIN POLYMORPHS, AND PROCESSES FOR PREPARATION THEREOF
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The invention provides Saxagliptin Schiff bases, polymorphs of Saxagliptin and (1S,3S,5S)-2-[(2S)-2-propan-2-ylideneamino-2-(3-hydroxy-1-adamantyl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile, processes for preparing Saxagliptin hydrates, and pharmaceutical compositions thereof.
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Page/Page column 10
(2011/11/13)
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- CRYSTAL FORMS OF SAXAGLIPTIN
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The present invention relates to novel polymorphic forms of Saxagliptin Hydrochloride. The present invention also relates to methods of making polymorphic forms of Saxagliptin Hydrochloride.
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Page/Page column 16
(2010/11/03)
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- CRYSTAL FORMS OF SAXAGLIPTIN AND PROCESSES FOR PREPARING SAME
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Physical crystal structures of a compound of the formula (I): are provided including the free base monohydrate thereof (form H-1) and the hydrochloric acid salt thereof, including hydrochloric acid salt containing 0.75 equivalent of H2O (form H0.75-3) and hydrochloric acid salt containing 2 equivalents of H2O (form H2-1), and hydrochloric acid salt Pattern P-5, preferably in substantially pure form, and other forms as described herein, pharmaceutical compositions containing structures of compound I or IA, processes for preparing same, intermediates used in preparing same, and methods of treating diseases such as diabetes using such structures.
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Page/Page column 33
(2008/12/08)
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