Monomethyl sulfate → 7-Amino-3-methoxymethyl-3-cephem-4-carboxylic acid

Participants

Reaction Conditions

Reaction Steps

16.7 g of a methanolic solution of methoxysulfonic acid (prepared as described in Preparation 2), 2.18 g of trimethyl borate and 2.45 g of methylal (prepared as described in Preparation 5) were added to 20 ml of sulfolane. The mixture was cooled to 10° C., and 2.74 g of 7-ACA were added thereto, followed by stirring at 10° C. for 1.5 hours. After completion of the reaction, the reaction mixture was treated following the procedures described in Example 2. 1.94 g (yield 79%) of the title compound were produced with high purity.

Provenance & Evidence