| abstract |
The invention relates to a method for synthesizing a sitagliptin intermediate. In the method, formula II is asymmetrically reductively aminated in a suitable organic solvent to obtain formula I with ammonia or ammonium salt in the presence of a chiral phosphorus-coordinated transition metal catalyst and an acidic additive. The R- or S-configuration of the stereocenter is represented by *, and the I of the R configuration can be used to prepare sitagliptin. The reaction formula is: Wherein R and R are each independently selected from hydrogen , C1 -C12 straight or branched chain alkyl, C3-C12 cycloalkyl, C2-C12 alkenyl, C2-C12 alkynyl, C7-C12 aryl alkane base. The method has high yield and ee% value, mild reaction conditions, simple operation, convenient purification, low production cost, environmental friendliness and suitability for industrialized production. |