The invention relates to the technical field of
organic synthesis, in particular to a preparation method of an N-BOC-
aniline derivative, which takes an
aniline derivative and di-tert-butyl
dicarbonate as reaction substrates,
sodium hydride as a reaction
reagent, 4-dimethylaminopyridine as a catalyst and
tetrahydrofuran solvent as a
solvent to carry out
amino acylation reaction to obtain the N-BOC-
aniline derivative. In the
amino acylation reaction process, the temperature is controlled to be 20-30 DEG C, the rotating speed is controlled to be 400-500 r / min, the obtained reaction liquid is purified to finally obtain the N-BOC-aniline derivative, the aniline derivative is 2-
bromine-5-chloroaniline, 4-hydroxyaniline, 3-hydroxyaniline, 4-carboxyl aniline, 3-carboxyl aniline or 4-
bromine-6-carboxyl aniline, and the N-BOC-aniline derivative is 2-
bromine-5-chloroaniline, 4-hydroxyaniline, 3-hydroxyaniline, 4-carboxyl aniline, 3-carboxyl aniline or 4-bromine-6-carboxyl aniline. The preparation method has the characteristics of simple preparation process, low preparation cost and high yield and purity of the final N-BOC-aniline derivative, the final yield can reach 84-93%, and the purity can reach 98.98-100%.