METHOD FOR PREPARING SITAGLIPTIN INTERMEDIATE VIA ASYMMETRICAL REDUCTION METHOD

摘要

Disclosed is a method for synthesizing a sitagliptin intermediate, the method comprising: under the existence of transition metal catalyst of chiral phosphine ligand and hydrogen, conducting asymmetrical reduction ammonification reaction on a formula II compound and ammonia salt or ammonium salt in a proper organic solvent under the condition of adding an acidic additive, and obtaining a formula I compound, wherein, a configuration of R- or S- of a stereocenter is represented by *; the formula I compound of R configuration can be used to prepare sitagliptin, and a reaction formula is as the following: R1 and R2 are respectively and independently selected from hydrogen, C1-C12 straight chain or branched-chain alkyl, C3-C12 cycloalkyl, C2-C12 chain alkenyl, C2-C12 chain alkynyl and C7-C12 arylalkyl. The method has a high yield and a high ee% value, a mild reaction condition and a low production cost, is simple to operate and convenient to purify, and is environmentally friendly and suitable for industrial production.