| 摘要 |
1320548 Nitrofuran derivatives SCHERING AG 15 July 1970 [19 July 1969] 34322/70 Heading C2C Novel compounds of Formula I in which R represents a dialkylamino group in which each alkyl group contains 1 to 5 carbon atoms or represents a pyrrolidino, piperidino, hexamethyleneimino, piperazino or morpholino group, each of which pyrrolidino, piperidino, hexamethyleneimino, piperazino and morpholino groups and the alkyl groups in the dialkylamino group may be substituted by an alkyl group containing 1 to 5 carbon atoms, an hydroxyl group, an acyloxy, acyl or hydroxyalkyl group each containing 1 to 5 carbon atoms or an acyloxyalkyl group in which the acyl and alkyl parts each contain 1 to 5 carbon atoms, aneach of which pyrrolidino, piperidino, hexamethyleneimino, piperazino and morpholino groups may be bridged by a -CH 2 -CH 2 - group, and their physiologically tolerable acid addition and quaternary ammonium salts, are prepared by nitrating a compound of Formula II in which R<SP>1</SP> is the same as R except that it contains no hydroxy groups, if desired, hydrolysing any ester group in the resulting compound and then, if desired, re-esterifying, and/or converting a free base into a salt, and/or converting a salt into a free base. Starting materials of Formula II are prepared by heating a reactive ester of the compound of Formula III with an amine of formula HR and then acylating any free hydroxy groups in the product in the usual manner. 2 - (2<SP>1</SP> - Furyl) - 5 - (2<SP>11</SP> - para - tolueneaulphonyloxy-ethoxy)-pyrimidine is prepared by reacting the compound of Formula III with p, toluenesulphonyl chloride. Pharmaceutical compositions having antibacterial and antitrichomonal activity, for oral, parenteral, topical or vaginal administration, comprise a compound of Formula I, or a physiologically tolerable acid addition or quaternary ammonium salt thereof, together with a pharmaceutical carrier. |
