酶法合成头孢克罗

Enzymatic synthesis of cefaclor from 7-aminodesacetoxymethyl-3-chlorocephalosporainc acid(6-ACCA) and phenylglycine derivatives using penicillin G acylase was studied .Many factors that affect the conversion of 7-ACCA to cefaclor were examined.The immobilized enzyme from Bacillis megaterium gave a better catalytic properties and the higher conversion was obtained using phenylglycine methyl ester(PGME) as acyl donor.And the external mass transfer limitation could be eliminated when the stirring rate was more than 150r/min.Low temperature was beneficial for the synthesis and the results showed that the synthetase activity was hardly influenced by temperature while the amidase activity was affected greatly by temperature.The optimum reaction conditions were determined at pH 6.5 and 10℃,respectively.The best 7-ACCA conversion of 56% was achieved when the intial concentration of 7-ACCA and PGME was at 50 mM and 150mM,respectively.

Kinetically Controlled Synthesis of Cefaclor using Penicillin G Acylase

Enzymatic synthesis of cefaclor from 7-aminodesacetoxymethyl-3-chlorocephalosporanic acid (7-ACCA) and phenylglycine derivatives using penicillin G acylase was studied. Many factors that affect the conversion of 7-ACCA to cefaclor were examined. The immobilized enzyme from Bacillis megaterium gave a better catalytic properties and the higher conversion was obtained using phenylglycine methyl ester (PGME) as acyl donor. And the external mass transfer limitation could be eliminated when the stirring rate was more than 150 r/min. Low temperature was beneficial for the synthesis and the results showed that the synthetase activity was hardly influenced by temperature while the amidase activity was affected greatly by temperature. The optimum reaction conditions were determined at pH 6.5 and 10 ℃, respectively. The best 7-ACCA conversion of 56% was achieved when the initial concentration of 7-ACCA and PGME was at 50 mM and 150 mM, respectively.