The invention discloses a
vildagliptin preparation method, and relates to the technical field of preparation of
pyrrolidine heterocyclic compounds. The method comprises the following steps: 1, preparing an
acetonitrile solution of S-1-chloroacetyl-2-cyanpyrrolidine; 2, adding
acetonitrile into a reaction kettle, stirring, adding 3-amino-1-adamantanol,
potassium carbonate and
potassium iodide, heating, adding the
acetonitrile solution of S-1-chloroacetyl-2-cyanpyrrolidine in a dropwise manner, and carrying out a heat insulation reaction after the dropwise addition until the reaction is completely carried out; and 3, post-
processing: cooling, stirring, centrifuging, collecting the obtained
filter cake, adding
dichloromethane into the kettle, stirring, adding the
filter cake, stirring, centrifuging, collecting the obtained filtrate, concentrating the filtrate to obtain a concentrate, re-crystallizing the concentrate by using isopropanol to obtain a crude product, carrying out hot washing on the crude product by using isopropanol, cooling, and centrifuging to obtain a product. The product is obtained through the one-step reaction by using the method, the yield is high, the
chemical purity and the chiral purity are respectively greater than 99%, and the method has the advantages of short reaction time, low
energy consumption and simple operation.