PURPOSE: To obtain a novel compound useful as an elastase inhibitor in the treatment of inflammation or degenerative diseases caused by protease.
CONSTITUTION: This novel compound is expressed by formula I (wherein (n) is 0-2; R1 is H, halogen, 1-4C alkyl or the like; R2 is H, 1-8C alkyl or the like; R3 is H, acetoxymethyl or the like; R4 is 1-8C alkyl, 2-6C alkenyl or the like; R5 is 6-10C aryl or heterocyclyl), e.g. 4-tert-butylcarbonyl-2,3-dimethyl-7α- methoxy-2-(1-methyl-1,2,3,4-tetrazol-5-yl)thio-3-cephem1,1-dioxide. The compound of formula I is obtained by allowing a compound of formula II (wherein n' is 0-2) and a compound of the formula, L-R4 (wherein L is a leaving group) to undergo alkylation reaction in the presence of a base (e.g. triethylamine) in a solvent (e.g. dimethylsulfoxide) at a temperature of from -60 to 40°C, and then, if required, converting it into a salt through oxidative reaction.
PIERURUIJI BITSUSORIINO
ETSUTOORE PEROONE
BINCHIENTSUO RITSUTSUO
