CEPHALOSPORIN COMPOUNDS AND PREPARATION PROCESS THEREOF

摘要

PURPOSE: Cephalosporin compounds and a preparation process thereof are provided, which compounds have strong antimicrobial activity, especially to methicillin resistant Staphylococcus aureus(MRSA). CONSTITUTION: Cephalosporin compounds represented by the formula (1) are provided, wherein A is hydrogen or amino protecting group; R1 is hydrogen, or C1-6 alkyl, C3-4 alkynyl, C3-6 cycloalkyl or C3-6 cycloalkyl-methyl containing 1 to 3 oxygen or halogen; R2 is hydrogen or carboxyl protecting group; Ar is one compound selected from one compound containing Y, W, R3, R4, R5 and R6 or one compound containing W, Y, z, R7, R8 and R9; R3, R4 and R7 are independently hydrogen, hydroxyl, C1-6 alkyl, C1-6 substituted or unsubstituted amino, C1-6 hydroxyalkyl or C1-6 alkylthio; R6 is hydrogen, hydroxyl, C1-6 alkyl substituted or unsubstituted amino, C1-6 alkyl or a compound containing I and J; I is S, NH, CH2 or O; n is 0, 1, 2, 3 or 4; J is C1-6 alkyl substituted or unsubstituted amino, hydroxy or C1-6 alkoxy; R8 and R9 are hydrogen, C1-6 alkyl, C1-6 alkylamino, hydroxy or C1-6 alkoxy; W and Y are independently N or C, provided that R3, R5 and R8 are not present when W or Y is N; Z is CH or N; Q is CH, C-G or N; G is halogen; and ethenyl positioned at the C-3 site where heteroarylthio is substituted may be present in the form of cis or trans.