Patent ID: 9006422
Filing Date: 2015-04-14
Classification: C07D

Abstract:
1. A process for the preparation of 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 1 is a hydroxyl protecting group and R 2 is a carboxylic acid protecting group, which process is characterized in that it comprises oxidizing a compound of formula (II) 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, mixtures of dichloromethane and tetrahydrofurane and mixtures of dichloromethane and acetonitrile.