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US 8,071,330 B2Granted
Process for the synthesis of cefaclor
AssigneeDsm IP Assets B.V.
InventorsHarold Monro Moody, Theodorus Johannes Godfried Maria Van Dooren
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AssigneeDsm IP Assets B.V.
InventorsHarold Monro Moody, Theodorus Johannes Godfried Maria Van Dooren
Estimating the term…
The present invention relates to a process for the synthesis of cefaclor, which process comprises reacting 7-amino-3-chloro cephalosporanic acid (7-ACCA) with D-phenylglycine in activated form (PGa) in the presence of an enzyme in a reaction mixture to form cefaclor, wherein at least part of 7-ACCA and/or PGa are added to the reaction mixture during the course of the reaction. The invention also relates to an aqueous mixture comprising an amount of cefaclor of >10 (w/w) %, an amount of 7-amino-3-chloro cephalosporanic acid of <2 (w/w) %, and an amount of D-phenyl glycine of <2 (w/w) % and a process for the recovery of cefaclor from this aqueous mixture. The invention also relates to cefaclor in crystal form having an absorbance at 400 nm (A400) of less than 0.250.
A process for the synthesis of cefaclor, said process comprising reacting 7-amino -3-chloro cephalosporanic acid (7-ACCA) and a mutant penicillin acylase of E. coli having a beta subunit wherein said mutant penicillin acylase has L-alanine substituted for L-phenylalanine at position 24 of the beta-subunit with added D-phenylglycine methyl ester in a reaction mixture at a pH of 7 to form cefaclor, wherein the added D-phenylglycine methyl ester is added at a constant rate for at least 90 minutes to the reaction mixture during the course of the reaction, wherein the added D-phenyl glycine methyl ester is added in a total amount to the reaction mixture in a 1.1 molar ratio to the 7-ACCA .
Dependencies are inferred from the claim text.