| 摘要 |
A process for the preparation of b-carboline related compounds for the formula as shown. The b -carboline related compounds are useful for treating symptoms of depression, psychosis, schizophrenia, phobia, anxiety, panic attacks, sleep disorders, appetite disorders, impulsive and aggressive disorders, sexual disorders, migraine. The compounds are potent selective ligands of 5-HT2 receptors, in particular 5-HT2c and 5HT2B antagonists. Wherein; R1 represents hydrogen, linear or branched C1-6alkyl, -R6-aryl, R6-cycloalkyl, R6-heterocycle, -COOR7, -COOR8, CONH-R8; wherein R6 is a linear or branched C1-6alkylene group, R7 is a linear or branched C1-6alkyl, aryl, cycloalkyl, heterocycle, -R6-cycloalkyl group or -R6-heterocycle, and R8 is hydrogen, a linear or branched C1-6alkyl, aryl, cycloalkyl, heterocycle, -R6-aryl, -R6-cycloalkyl or -R6-heterocycle; R2 represents -CN, -COOR8, -CONHR8, mono-C1-6alkylamino-C1-6alkylaminocarbonyl, di-C1-6alkylamino-C1-6alkylaminocarbonyl, -NR8R9, -NHCOOR7, -COR8 or R3 and R4 together form C3-10cycloalkyl group; R5 represents hydrogen, linear or branched C1-6alkyl group or an aryl-C1-6alkyl group in which the alkyl moiety may be linear or branched; Ra, Rb, Rc and Rd, which may be-identical or different, each represents, independently of the others, a group selected from hydrogen, halogen, linear or branched C1-6alkyl, hydroxy, linear or branched C1-6alkoxy, linear or branched trihalo-C1-6alkyl, linear or branched trihalo-C1-6alkoxy, nitro, cyano, amino, linear or branched C1-6alkylamino, di-C1-6alkylamino in which each alkyl moiety may be linear or branched, aryl, aryl-C1-6alkyl in which the alkyl moiety may be linear or branched, carboxy, linear or branched C1-6alkylcarbonyloxy, linear or branched C1-6acyl, aryloxy, and aryl-C1-6alkoxy in which the alkoxy moiety may be linear or branched.
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