The invention discloses a synthesis method of 5-amino-8-
formic acid-3, 4-dihydroisoquinoline-2, 8 (1H)-
carboxylic acid tert-butyl ester, and relates to the technical field of
organic synthesis. The synthetic method provided by the invention comprises the following steps: (1) carrying out
carbonylation reaction on 5-amino-8-bromo-2-tert-butyloxycarbonyl-1, 2, 3, 4-
tetrahydroisoquinoline, [1, 1 '-bis (diphenylphosphino)
ferrocene]
palladium dichloride and
carbon monoxide to obtain 5-amino-8-
methyl formate-3, 4-dihydroisoquinoline-2, 8 (1H)-
carboxylic acid tert-butyl ester; and (2) carrying out
saponification reaction on the 5-amino-8-
formic acid-3, 4-dihydroisoquinoline-2, 8 (1H)-
carboxylic acid tert-butyl ester and
sodium hydroxide to obtain the 5-amino-8-
formic acid-3, 4-dihydroisoquinoline-2, 8 (1H)-carboxylic acid tert-butyl ester. According to the invention, 5-amino-8-bromo-2-tert-butyloxycarboryl-1, 2, 3, 4-
tetrahydroisoquinoline,
sodium hydroxide and the like are taken as raw materials, the 5-amino-8-formic acid-3, 4-dihydroisoquinoline-2, 8 (1H)-carboxylic acid tert-butyl ester is synthesized through a two-step reaction, the synthesis path is short, the synthesis method is simple, and the product yield is high.