NEW MATERIAL:The compound of formula I (R1 is H or methyl; R2 and R3 are H, lower alkyl or together with adjacent N form aziridinyl, azetidinyl, pyrrolidinyl, piperidino, piperazinyl or morpholino; A is carbonyl or single bond; n is 0-3), its salt or ester.
EXAMPLE: (5R,6S)-2[(2S,4S)-2-[2-(N, N-dimethylaminocarbonyl)- cyclopropyl]pyrrolidin-4-ylthio]-6-[(R)-1-hydroxyethyl]-1-carbapen-2-em-3- carboxylic acid.
USE: An antibacterial agent. It has strong antibacterial action against sensitive and resistant Gram-positive bacteria and Gram-negative bacteria and excellent stability to β-lactamase and DHP-1.
PREPARATION: The objective compound of formula I can be produced by reacting a compound of formula II (R4 is H or COOH-protecting group; R5 is H or OH-protecting group) with a compound of formula III (R20 and R30 are R2, R3 or amino- or imino-protecting group) and, as necessary, deprotecting the reaction product.
YAMADA KOJI
USHIJIMA RYOSUKE
Next Patent: 4-AMINO-5,6,7,8-TETRAHYDROTHIENO(2,3-B)QUINOLINE DERIVATIVE