1-βMETHYLCARBAPENEMCARBOXYLIC ACID ESTER DERIVATIVE AND METHOD FOR PREPARATION THEREOF

摘要

PURPOSE: Provided is a 1-βmethylcarbapenemcarboxylic acid ester derivative wherein lactam is linked to hydroxymethyl at C-2, which has high antibiotic effects on both gram positive and negative bacteria except for Pseudomonas aeruginosa. Also, its preparation method is provided. CONSTITUTION: 1-βmethylcarbaphenemcarboxylic acid ester derivative is represented by the formula(1), wherein R1 is hydrogen atom or cyclic or noncyclic low alkyl having C1-C4; R2 is pivaloyloxyalkyl, low alkoxycarbonyloxyalkyl or alkyldioxoleneonalkyl having C1-C6; and n is 1-3. It is prepared by reacting 1-βmethylvcarbephenem derivative represented by the formula(2), wherein R1, R2 and n is as described above; R is hydrogen or anion induced from organic or inorganic salt; and X is halogen with halide represented by the formula(3) of X-R2 or sulfonate compound.