Substituierte (Nitrofurylacryliden)-hydrazine und Verfahren zu deren Herstellung

摘要

1367203 (Nitro-furylacrylidene)-hydrazine derivatives LIPHA LYONNAISE INDUSTRIELLE PHARMACEUTIQUE 6 Jan 1972 [7 Jan 1971] 685/72 Heading C2C Novel nitrofuran derivatives of general Formula I in which n is 0 or 1, G is a furoyl, thenoyl, nitrothenoyl or carbobenzyloxy and R is hydrogen, methyl, n-butyl, isobutyl, hydroxymethyl, benzyl, p-hydroxybenzyl or 8-(2-furoyl)-aminobutyl are prepared by reacting a 5-nitro-2- furyl-acrolein with a substituted hydrazide G-(NH-CH(R)-CO) n -NH-NH 2 (II) preferably in an organic solvent and with an acid catalyst. Compounds of Formula I include [N1 - (51 - nitro - 21 - thenoyl) - N2 - (511 - nitro- 211-furyl-acrylidene]-hydrazine and [N1-(51-nitro- 21 - thenoyl - glycyl) - N2 - (511 - nitro - 211 - furylacrylidene]-hydrazine. Compounds of Formula II are prepared by reacting an amino ester G-(NH-CH(R)- CO) n -OEt (III) with hydrazine. Compounds of general Formula III in which n is 0 are prepared by reacting an amino ester NH 2 -CH(R)-COOEt(IV) with an acid chloride G-Cl in the presence of an alkali agent. Compounds I of formula have antibacterial activity and form with a carrier or excipient a pharmaceutical composition which may be administered orally or topically.