NEW CPHALOSPHORIN COMPOUND FOR ORAL ADMINISTRATION AND PREPARATION METHOD THEREOF

摘要

PURPOSE: A cephalosporin compound as antibiotic is provided which has strong antibiotic action against various pathogens including gram negative bacteria, also can be orally administered without degrading its efficiency. CONSTITUTION: The compound of formula (1a) is obtained by (a) reacting the compound of formula (5a) with the compound of formula (6a) in the presence of base, or (b) reacting the compound of formula (5b) with the compound of formula of (6b), or (c) reducing S → oxide of the compound of formula (1a) in which m is 1. In Formula (1), A is amino guard radical. R1 is hydrogen, or C3-4 alkinyl radical substituted or non-substituted by C1-6 alkyl radical which can be substituted one to three by C1-6 alkoxy, cyano, halogen, C3-6 cyclo alkyl or C5-6 hetero aryl containing one to two of nitrogen atom or oxygen atom, C3-4 alkenyl radical, and amino, or C3-6 cyclo alkyl radical. R2 is hydrogen or carboxyl guard radical. U is hydrogen, or substituted or non-substituted amino radical. V and W are C or N,respectively. Y and Z are a substituted or non-substituted amine radical, hydroxyl radical, or C1-4 alkyl radical, respectively. Q is CH, CX, or N, wherein X is halogen.