摘要:
A process for producing an azulene derivative useful as a Na+-glucose cotransporter inhibitor, which is high in yield, is simple in operation, is low in cost, is suited for environmental protection, and is advantageous industrially, the process being characterized by reducing and deprotecting at least one compound selected from penta-acyl compounds and tetra-acyl compounds or salts thereof to obtain a C-glycoside compound; and a useful intermediate for synthesis of such an azulene derivative, obtained in the course of the above process.
摘要:
A process is provided for preparing a tetrahydrobenzimidazole derivative represented by Formula (Ib): ##STR1## wherein Het representa s heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxycarbonyl group, and a halogen atom; and X.sup.2 represents a single bond connected to the carbon atom of the heterocyclic ring as represented by Het. The process comprises reacting a heterocyclic compound represented by Formula (IIIa):Het--X.sup.2 --H (IIIa)wherein Het and X.sup.2 are as defined above, with a carboxylic acid represented by Formula (II): ##STR2## or a reactive derivative thereof.
摘要:
4,5,6,7-Tetrahydrobenzimidazole derivatives represented by general formula (I) ##STR1## wherein groups represents the following: R.sup.1, R.sup.2, R.sup.3 : independently represent hydrogen atom, hydroxy group, a halogen atom, a lower alkyl group which may optionally be substituted with a halogen atom, a lower alkoxy group, a lower alkylthio group, an aralkyloxy group, an aryloxy group, a lower alkanoyl group, carboxy group, a lower alkoxycarbonyl group or nitro group;R.sup.4, R.sup.5, R.sup.6 : hydrogen atom or a lower alkyl group;X: oxygen atom or sulfur atom;or salts thereof which are believed to have a 5-HT.sub.3 antagonizing activity.
摘要:
A tetrahydrobenzimidazole derivative represented by formula (I): ##STR1## wherein Het represents a heterocyclic group which may be substituted with 1 to 3 substituents selected from the group consisting of a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl-lower alkyl group, an aralkyl group, a lower alkoxy group, a nitro group, a hydroxyl group, a lower alkoxycarbonyl group, and a halogen atom; and X represents a single bond or --NH-- which is bonded to the carbon atom or nitrogen atom of the heterocyclic ring, or a pharmaceutically acceptable salt thereof.The compound of formula (I) and a salt thereof exhibits antagonism against 5-HT.sub.3 receptor.