1-Amino-7-methoxy-β-carboline (2) was synthesized through Curtius rearrangement and alkaline hydrolysis from 1-azidocarbonyl-7-methoxy-β-carboline, which was obtained from 1-methoxycarbonyl- 7-methoxy-β-carboline (4) via hydrazinolysis and diazotization reactions. A series of 1-alkoxycarbony- lamino derivatives 3 of compound 2 were prepared by reaction of 6 in the presence of alkyl alcohol in a re-flux condition. All the compounds were identified by 1H NMR, 13C NMR, MS techniques and elemental analysis. The preliminary antitumor activities were investigated by MTT method and the results show that the synthesized compounds display somewhat antitumor activity at the concentration of 10－5 mol/L. The in-hibition rates of 3e, 3g and 3h against HepG2 and SGC-7901 cells were higher than that of harmine (1), which was used as a positive control drug.

Key words: synthesis, β-carboline, 1-amino-7-methoxy-β-carboline, derivative, antitumor acitivity