Synthesis of the main related material of vildagliptin and its optimization / 国际药学研究杂志

ABSTRACT

Objective To synthesize the impurity of vildagliptin as a reference substance, and optimize its preparation process by the central composite design-response surface methodology. Method The impurity was synthesized from L-proline and 3-amino-1-adamantanol through chloroacetylation, amination, dehydration and substitution. Results The structure of the disubstituted derivative of vildagliptin was verified by IR, 1H-NMR and MS. Conclusion The synthesized compound can be used as the reference substance of the impurity, so the impurity can be controlled. Preparation process gained the application value after it was optimized by the central composite design-response surface methodology.