- A preparation method of advantage geleg sandbank (by machine translation)
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The invention relates to a preparation method of Linagliptin. According to the preparation method, potassium carbonate or sodium carbonate is taken as an alkali; an iodine-containing inorganic salt is taken as a catalyst; N-methyl-2-pyrrolidone (NMP) or N,N-Dimethylformamide (DMF) is taken as a solvent; 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1H-purine-2,6-dione is reacted with a (R)-3-aminopiperidine compound firstly at 40 to 50 DEG C; after reaction, 2-(chloromethyl)-4-methylquinazoline is directly added for reaction so as obtain a compound D; and the compound D is subjected to step 1-2 to prepare Linagliptin. The preparation method is capable of shortening reaction time, and increasing yield.
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Paragraph 0048; 0049
(2018/08/03)
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- Synthesis and characterization of process-related impurities of antidiabetic drug linagliptin
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Linagliptin, a xanthine derivative, is a highly potent, selective, long-acting and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. During the process development of linagliptin, five new process-related impurities were detected by high performance liquid chromatography (HPLC). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, HRMS, 1H-NMR, 13C-NMR and IR) as described in this article. The identification of these impurities should be useful for quality control and the validation of the analytical method in the manufacture of linagliptin.
- Huang, Yiwen,He, Xiaoqing,Wu, Taizhi,Zhang, Fuli
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- METHOD FOR PREPARING AN IMPORTANT INTERMEDIATE OF LINAGLIPTIN
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The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.
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- METHOD FOR PRODUCING CHIRAL 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES
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The invention relates to an improved method for producing enantiomer-free 8-(3-amino-piperidin-1-yl)-xanthines.
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Page/Page column 10-11
(2008/06/13)
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