| abstract |
The invention discloses a preparation method of optically active 3-aminopiperidine and its derivatives, and its application in the synthesis of dipeptidyl peptidase-IV inhibitor linagliptin. In the preparation method, 3-aminopyridine is used as a raw material, and compound I is obtained by protecting the 3-amino group, reducing the pyridine ring by catalytic hydrogenation, and splitting with a chiral reagent, and then deprotecting to obtain (R)-3-aminopiperidine Hydrochloride II. In the application, compound III prepared from compound I is an important intermediate for synthesizing linagliptin, and (R)-3-aminopiperidine hydrochloride II can also directly synthesize high-purity linagliptin. The raw materials used in the invention are low in price, easy to obtain in the market, simple in unit operation of each step, low in equipment requirements, high in safety, and easy in industrialized production. |