ABSTRACT
Objective To optimize the process of vildagliptin based on the principle of quality by design(QBD),so as to con?trol the safety and quality of the product. Methods Process route was confirmed through investigating literature and the advantages or disadvantages of each route were discussed. The key process parameters were determined according to the single factor experiments , which were designed by understanding of product process and process controls. Meanwhile,impurities of intermediates were studied and the safety and quality of the product could be guaranteed. Results and Conclusion Industrial process of vildagliptin was devel?oped by the principle of QBD,which can promise the safety and quality of vildagliptin,improve product quality and meet the registra?tion requirements of State Food and Drug Administration(SFDA).
ABSTRACT
Isavuconazole is a broad-spectrum triazole antifungal agent,which is administered as a water-soluble prodrug-isa?vuconazonium sulfate. Recently,its oral and intravenous formulations are available. Isavuconazole inhibits fungal cytochrome P45014DM,thus interferes with the biological function of cell wall formation and plays the antifungal role. In this paper ,we summa?rize the synthetic methods of isavuconazole ,water-soluble segments of side chain and isavuconazonium sulfate and evaluate their advantages and disadvantages,which lays a foundation for isavuconazonium sulfate technology development.
ABSTRACT
Vildagliptin is a kind of dipeptidyl peptidase Ⅳ(DPP-4) inhibitors. It is a new oral diabetes drug which is developed by Novartis. It reduces blood glucose levels by decreasing the concentration of glucagon,has remarkable advantages in drug safety and is widely used in the treatment of type 2 diabetes in clinic. In this paper,we summarize the synthetic methods of vildagliptin that have been reported in literature in recent years and their advantages and disadvantages.