合成路线1

By cyclization of 6-bromo-1H-indole-3-carbothioamide (V) with 6-bromo-3-(2-bromoacetyl)-1-tosyl-1H-indole (VIII) in refluxing ethanol, followed by elimina-tion of the tosyl protecting group with NaOH in refluxing methanol. The intermediates 6-bromo-1H-indole-3-carbothioamide (V) and 6-bromo-3-(2-bromoacetyl)-1-tosyl-1H-indole (VIII) have been obtained as follows: 6-Bromo-1H-indole-3-carbothioamide (V): The reaction of 6-bromoindole (I) with POCl3 and DMF, followed by hydrolysis with NaOH in refluxing water gives 6-bomoindole-3-carbaldehyde (II), which is treated with propyl nitrite and diammonium phosphate in refluxing acetic acid to yield the nitrile (III). Finally, the reaction of (III) with thioacetamide and HCl in refluxing DMF affords the interme-diate carbothioamide (V). 6-Bromo-3-(2-bromoacetyl)-1-tosyl-1H-indole (VIII): The protection of 6-bromoindole (I) with tosyl chloride and NaOH in toluene/water gives the 6-bromo-1-tosylindole (VI), which is acetylated with acetic anhydride and AlCl3 in dichloro-methane yielding the 3-acetyl derivative (VII). Finally, the bromination of (VII) with CuBr2 in refluxing ethyl acetate/chloroform affords the target 3-(bromoacetyl) derivative (VIII).