PROCESS FOR PREPARING -LACTAM-CONTAINING ANTIBACTERIAL AGENTS

Penems I (R=H, lower alkyl, 2,2,2-trichloroalkyl, benzyl, acetonyl, p-nitrobenzyl, p-methoxybenzyl, Ph, p-nitro-Ph, benzhydryl, acetoxymethyl, Me-CH-OCO2Et, CH2NHCOR2; R2=C1-C5 alkyl, aryl; Z=H, halo, OH, amino, carbamoyloxy, mercapto, pyridinium, OR3, OCOR3, NHCOR3, SR4; R3, R4 independently=lower...

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Hauptverfasser: FOGLIO MAURIZIO, SANFILIPPO AURORA, ARCAMONE FEDERICO, SCARAFILE COSIMO, FRANCESCHI GIOVANNI
Format: Patent
Sprache:eng ; kor
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Zusammenfassung:Penems I (R=H, lower alkyl, 2,2,2-trichloroalkyl, benzyl, acetonyl, p-nitrobenzyl, p-methoxybenzyl, Ph, p-nitro-Ph, benzhydryl, acetoxymethyl, Me-CH-OCO2Et, CH2NHCOR2; R2=C1-C5 alkyl, aryl; Z=H, halo, OH, amino, carbamoyloxy, mercapto, pyridinium, OR3, OCOR3, NHCOR3, SR4; R3, R4 independently=lower alkyl, aryl, heterocyclic ring; n=0, 1) were prepd. Thus, 2.0g methylpenicillinate S-oxide in 40mL toluene and 2.8g butandiol diacetate were refluxed for 24 hrs. to give 1.4g 4β-vinylthio - [1,2-diacetoxymethyl - 1 - [methoxycarbonyl-2-methyl-2-propenyl - azetidine-2-on-S-oxide.