Patent ID: 9499566
Filing Date: 2016-11-22
CPC Classification: C07D

Claim Text:
1. A process for the preparation of ceftobiprole in form of its water-soluble prodrug ceftobiprole medocaril, comprising the steps of: (1) preparing 7-[2-(5-amino-[1,2,4]thiadiazol-3-yl)-2-hydroxy-imino-acetylamino]-3-formyl-8-oxo-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid derivative of formula (I): wherein R with a combination of a hypervalent iodine oxidizing agent of the type 10-I-3 and a catalyst selected from 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO), 4-hydroxy-2,2,6,6-tetramethyl-1-piperidinyloxy and 4-(acetylamino)- 2,2,6,6-tetramethyl-1-piperidinyloxy in a solvent selected from the group consisting of dichloromethane, a mixture of dichloromethane and tetrahydrofurane and a mixture of dichloromethane and acetonitrile; and (2) synthesizing said ceftobiprole medocaril from said compound of formula (I).