| 摘要 |
PROBLEM TO BE SOLVED: To obtain a new beta-carboline compound which is a strong ligand for a 5-HT2 receptor that is one of the family of 5-hydroxytryptamine (5-HT) receptors and is useful for treating depression, psychosis, somnipathy, aggressive lesion, and so on. SOLUTION: A compound of formula I [the dotted line is a single bound or a double bond (for giving an aromatic property to a ring which has the dotted line); R1 is H. COR8 (R8 H, an aryl or the like) or the like; R2 is cyano, CO2R8 or the like; R3 and R4 together form a 3 to 10C cycloalkyl; R5 is H, a 1 to 6C alkyl or the like; Ra to Rd are each H, a halogen, OH or the like], for example, cyclopentyl 1-(6-chloro-2,3,4,9-tetrahydro-1H-β-carbolin-1-yl) cyclobutanecarboxylate. The compound of formula I is produced, for example, by reacting a compound of formula II with a compound of formula III and then treating the obtained compound of formula IV in the presence of phosphorus oxychloride in a solvent (for example, toluene) to obtain a compound of formula V.
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