| 摘要 |
<p>PURPOSE:To obtain a new pyridoindole derivative useful as a strong and selective antagonist of 5-HT acceptor. CONSTITUTION:A compound shown by formula I (R<1> and R<2> are H or lower alkyl; m and n are 0-2) or a pharmaceutically acceptable salt such as 8,9- dihydro-10-methylpyrido[1,2-a]indole-6-(7H)-one-7-spiro-6',7'-dihydro- 1'-methyl-5'H- pyrrolo[1,2-c]imidazole. The compound is obtained by reacting a compound shown by formula II (R<3> is imino-protecting group) with a halogenating agent such as thionyl chloride, phosphorus oxychloride or phosphorus pentabromide and subjecting the imino-protecting group of a prepared compound shown by formula III to elimination reaction (e.g. hydrolysis or reduction). The compound is effective for treating and preventing mental disease, central nerve disorder, ache, gastrointestinal disorder, unpleasantness, vomiting, kinesia, etc.</p> |
