公开(公告)号：EP4050102A1

公开(公告)日：2022-08-31

申请号：EP21884273.0

申请日：2021-01-21

申请人： Zhejiang Yongtai Technology Co., Ltd. ,  Zhejiang University of Technology ,  Zhejiang Yongtai Pharmaceutical Co., Ltd.

发明人： LIU, Zhiqiang ,  CHENG, Feng ,  ZHANG, Xiaojian ,  JIA, Dongxu ,  ZHENG, Yuguo ,  HE, Renbao ,  JIN, Yizhong ,  SHAO, Hongming ,  LIN, Jiaohua ,  ZHANG, Feng

IPC分类号： C12N9/10 ,  C12N15/54 ,  C12N1/21 ,  C12N15/63 ,  C12P17/12

摘要： The present invention discloses a transaminase mutant and application thereof in preparation of sitagliptin intermediates, the transaminase mutant is obtained by substitution of tyrosine with proline at position 74, substitution of glutamic acid with aspartic acid at position 228, substitution of leucine with alanine at position 254 and substitution of methionine with threonine at position 290 of the amino acid sequence shown in SEQ ID NO: 2. The present invention uses wet cells or a purified transaminase as a biocatalyst and a sitagliptin precursor ketone or a prochiral carbonyl compound as a substrate to prepare a sitagliptin intermediate or a sitagliptin ester intermediate; the total yield of the method reaches about 82%, and e.e. value of the product reaches 99%.