PROCESS FOR PRODUCING 7-AMINO-CEPH-3-EME-4-CARBOXYLIC ACID DERIVATIVES
摘要
A process is disclosed for preparing derivatives of 7-amino-cephalosporanic acid and 7-amino-desacetoxycephalosporanic acid of structure: <IMAGE> (V) starting from a 3-acylamino-2 beta -thiohydrazoazetidinone of structure: <IMAGE> (II') wherein the compound (II') is reacted with a phosphorous halide in the presence of a tertiary amine, the corresponding imino chloride is reacted with a lower aliphatic alcohol, the iminoether so formed is hydrolyzed with water in an acid medium, and the resultant 3-amino-2 beta -thiohydrazoazetidinone of structure: <IMAGE> (IV') is reacted in a suitable solvent and at a temperature between -100 DEG and +120 DEG C with a compound selected from the class consisting of inorganic basic or weakly acid oxides and inorganic and organic bases, to finally give the desired compound (V) which is isolated and purified in known manner.
