| 摘要 |
1,236,634. Nitrofuran derivatives. SCHERING A.G. 24 June, 1968 [23 June, 1967], No. 29965/68. Heading C2C. Novel 5-nitrofuran derivatives of Formula (I) in which R represents an alkyl, cycloalkyl, alkoxy or cycloalkoxy group containing up to 6 carbon atoms which may be interrupted by an oxygen atom and/or substituted by a hydroxy or acyloxy group or by a halogen atom, or represents an aryl or aralkyl group which may be substituted by a chlorine atom or by a nitro, amino, alkyl or alkoxy group, or represents a hetero-aromatic group, and X represents a direct bond or a group of the formula -CH=CY- in which Y represents a hydrogen atom or a C 1-5 alkyl, aryl or aralkyl group, are prepared (a) when X represents a direct bond, by subjecting 5-nitro-2-amidinofuran or 2-amidino-furan, or an acid addition salt thereof, to a ring closure condensation with a #-dialkylamino-acrolein derivative of Formula (II) or (b) when X represent a group of formula -CH=CY-, by condensing at an elevated temperature and in the presence of a condensing agent 5-nitrofurfural or furfural, or a functional derivative thereof, with a compound of Formula (III) and, if necessary or desired, in the resulting compound introducing a nitro group into the 5-position of the furan nucleus, or replacing any hydroxy group by a halogen atom or esterifying any hydroxy group, or saponifying any acyloxy group. 2 - Methyl - 5 -methoxy-pyrinidine is prepared from acetamidine and α-methoxy-#-dimethylamino-acrolein. Antibacterial and antitrichomonal compositions for oral or topical administration comprise a compound I and a pharmaceutically suitable carrier. |
