Cephalosporin compositions and methods of manufacture

摘要

Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising the conversion of a protected 7-amino group into a 7-carboxamide moiety in a single step.

主权项

1. A method for preparing a compound of formula (II), or a salt thereof, comprising the step of reacting a compound of formula (III), or a salt thereof, with a compound of formula (IV), or a salt thereof, in a mixture comprising an organic solvent and water, to form a compound of formula (II), or a salt thereof; wherein: R1 is selected from the group consisting of:wherein Z′ is independently hydrogen or an oxygen protecting group;
Y is selected from the group consisting of:wherein R′ is selected from the group consisting of hydrogen and an oxygen protecting group;
R2 is hydrogen; R3 is selected from the group consisting of hydrogen and an oxygen protecting group; and R4 and R4, are each independently selected from the group consisting of: and —CH═CH2, wherein each occurrence of A is independently an anion, and X is —OSO2R8, wherein R8 is methyl.