| 摘要 |
<p>5-(Py-Y)-1H-benzimidazol-2-ol or 5-(Py-Y-1H-benzimidazole-2-thiol or lower-alkyl ethers or thioethers thereof or pharmaceutically-acceptable acid-addition salts thereof where Y is a direct linkage or lower-alkylene having one or two carbon atoms and Py is 4- or 3-pyridinyl, optionally having one or two lower-alkyl substituents, or 1-oxide of such pyridinyl, useful as cardiotonics, are prepared by reacting 4-(Py-Y)-1,2-benzenediamine with urea or carbony-Idiimidazole to produce 5-(Py-Y)-1H-benzimidazol-2-ol or with thiourea, an alkali metal lower-alkyl xanthate orthiocar- bonyldiimidazole to produce 5-(Py-Y)-1H-benzimidazole-2-thiol and by reacting 5-(Py-Y)-lH-benzimidazole-2-thiol with a lower-alkylating agent to produce 2-(lower-alkylthio-)-5-(Py-Y)-1 H-benzimidazole. 2-(Lower-alkoxy)-5-(Py-Y)-1 H-benzimidazoles are prepared by reacting 4-(Py-Y)1,2-benzenediamine with tetra-(lower-alkoxy)methane. The N-oxides may be prepared by reaction with a per-organic acid in a suitable solvent.</p> |
