Complexants for the clathration mediated synthesis of the antibiotic cephradine

Enzymatic synthesis of cephalosporins is hampered by secondary hydrolysis a nd by complicated down-stream processing. Instantaneous removal of cephalos porin product by clathration, using an efficient and selective complexing a gent, offers an attractive opportunity to tackle these problems. A series o f benzene derivatives that form clathrate-type complexes with the cephalosp orin antibiotics was subjected to efficiency measurements with Cephradine a nd enzyme inhibition studies. The best results for the antibiotic Cephradin e were obtained with methyl 2-aminobenzoate, 2-hydroxybiphenyl and methyl 4 -hydroxybenzoate. These three compounds are environmentally and toxicologic ally fully acceptable for application in a 'green' process.