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Synthesis and synthetic process optimization of a specific dipeptidyl peptidase-Ⅳinhibitor vildagliptin / 国际药学研究杂志
Journal of International Pharmaceutical Research ; (6): 677-682, 2020.
Artigo em Chinês | WPRIM | ID: wpr-845151
ABSTRACT

Objective:

To investigate and optimize the synthetic process of specific dipeptidyl peptidase-Ⅳ(DPP-Ⅳ)inhibitor vitagliptin.

Methods:

The aimed synthetic route was conceived by the literature survey according to the advantages and disadvantages of the reported synthetic routes. The key process parameters were determined by the orthogonal test or single factor test for the main intermediates in the speed limiting step.

Results:

The structures of intermediates and target compound were confirmed by MS and 1H NMR data. The overall yield of the target compound was 38.5%.

Conclusion:

The synthetic process has the advantages of lower cost, simple operation and mild reaction condition, and the yield has been improved by optimizing the crystallization solvent, which should be more suitable for industrial production.

Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Idioma: Chinês Revista: Journal of International Pharmaceutical Research Ano de publicação: 2020 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Idioma: Chinês Revista: Journal of International Pharmaceutical Research Ano de publicação: 2020 Tipo de documento: Artigo