| 摘要 |
PURPOSE: The method for producing beta-lactam antibiotics using enzymatic acylation is provided, thereby the beta-lactam antibiotics can be simply and cheaply produced using enzymes. CONSTITUTION: The beta-lactam antibiotics represented by formula (3) is produced by acylation reacting a compound represented by formula (1) with a compound represented by formula (2) using enzyme penicillin amidase, in which, R1CO is diphenyl glycine or dipara hydroxyphenyl glycine, X is OR2 or NR3R4, wherein R2 is C1 to C7 alkyl or haloalkyl, and R3 and R4 are individually hydrogen or C1 to C3 alkyl, and the penicillin amidase is derived from E. coli, Acetobacter pasteurianum, Xanthomonas citri, Kluyveri citrophylla or Bacillus megaterium. The beta-lactam antibiotics represented by formula (5) is produced by acylation reacting a compound represented by formula (4) with a compound represented by formula (2) using enzyme penicillin amidase, in which Z is hydrogen, halogen, C1 to C3 alkyl, C2 to C4 alkenyl, nuclear philic group-substituted C1 to C3 alkyl; R1CO is diphenyl glycine or dipara hydroxyphenyl glycine; X is OR2 or NR3R4, wherein R2 is C1 to C7 alkyl or haloalkyl, and R3 and R4 are individually hydrogen or C1 to C3 alkyl.
|
