CARBAPENEM ANTIBACTERIAL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT

摘要

PURPOSE: Carbapenem antibacterial compounds and a preparation method thereof are provided, in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH2 group and the naphthosultam is further substituted with various substituent groups including at least one cationic group. CONSTITUTION: The carbapenem antibacterial compounds are represented by the formula 1. These compounds are prepared by reacting a suitably protected 2-hydroxymethyl-carbapen-2-em-3-carboxylate having an active hydroxymethyl group at the 2-position with a suitably substituted naphthosultam in the presence of a suitable active reactant such as azodicarboxylate, triphenylphosphine, diisoprypylazodicarboxylate and tributylphosphine, to link the two starting materials through methylene group; and deprotecting and purifying the product.