| 摘要 |
1-R1-3-[unsubstituted, amino, cyano, carbamyl, halo, lower- alkylamino, di-(lower-alkyl)amino, lower-acylamino carboxy or lower- carbalkoxy]-6-(lower-alkyl)-5- (optionally lower-allyl substituted pyridinyl)-2(1H)-pyridinones or pharmaceutically- acceptable acid-addition or cationic salts thereof are useful as cardiotonic agents, where R1 is hydrogen, lower-alkyl or lower- hydroxyalkyl. 1-R1-3-amino-6-(lower- alkyl)-5-(pyridinyl)-2(1H)-pyridinones are prepared by hydrolyzing the corresponding 3-cyano compounds to produce the corresponding 3-carbamyl compounds and reacting the latter with a reagent capable of converting carbamyl to amino. The 1-R1-3-cyano-6- (lower-alkyl)-5-(pyridinyl)-2(1H)- pyridinones are prepared by reacting (pyridinylmethyl) lower-alkyl ketones with dimethylformamide di-(lower- alkyl)acetal to produce 1-(pyridinyl)-2- (dimethylamino)ethenyl lower-alkyl ketones and reacting said ketones with N-R1-O-cyanoacetamide to produce the 1-R1-3-cyano-6-(lower-alkyl)-5- (pyridinyl)-2(1H)-pyridinones. Also shown are the conversions: of the 3- cyano compounds to the 3-H and 3- carboxy compounds; of the 3-H compounds to the 3-halo compounds; of the 3-halo compounds to the 3-[mono- (lower-alkyl)-or di-(lower-alkyl)- amino]compounds; of the 3-amino compounds to the 3-lower-acylamino or 3-[mono-(lower-alkyl)- or di-(lower- alkyl) amino] compounds, and of the 3-carboxy compounds to the 3- carbethoxy compounds. |
