The invention discloses a synthesis method of furatadone, which comprises the following steps: by taking 1-(4-morpholinyl)-2-
propyne as a
raw material, carrying out [3 + 2]
cycloaddition reaction on the 1-(4-morpholinyl)-2-
propyne and di-tert-butyl azodicarboxylate to obtain a 3, 5-disubstituted
oxazolone intermediate; then under the action of a Pd / C catalyst, carrying out a
hydrogenation reaction of olefin to obtain N-Boc protected AMOZ; finally, the AMOZ protected by N-Boc and 5-nitrofurfural are subjected to a
condensation reaction under the action of
hydrogen chloride, and the product
furaltadone is obtained. The synthesis method is simple,
environmentally friendly and suitable for large-scale production.