The esterification of potassium phenoxymethylpenicillanate (I) with chloromethyl methyl ether (A) in methylene chloride-THF gives the methoxymethyl ester of penicilline V (II), which is then treated with dimethylaniline (B) in CH2Cl2 to afford methoxymethyl 6-aminopenicillanate (III). Finally, this product is condensed with phenylglycyl chloride (C) hydrochloride and acetone (D) by means of NaOH.