The invention discloses a
gram-level synthesis method of Dactyllactone A. The
gram-level synthesis method of Dactyllactone A is shown in the description. The method comprises the following steps: with simple and easily available
aryl iodide,
aziridine and triisopropyl silylacetylene as starting materials, stirring and reacting in an
organic solvent at 60-70 DEG C under the action of a
palladium catalyst, a
phosphine ligand, a
norbornene derivative and alkali to obtain a key intermediate; the key intermediate is condensed with iodo gem-
dimethyl ester furanone prepared from
propiolic acid and
dimethyl malonate iodine ylide, and then the condensation product is subjected to an Au / Ag catalyzed intramolecular
hydroamination reaction, photocatalytic 6-pi electro-cyclization and two-step conversion, so that the
natural product Dactyllactone A can be obtained, wherein the iodo gem-
dimethyl ester furanone and iodo gem-
dimethyl ester furanone are prepared from
propiolic acid and
dimethyl malonate iodine ylide. The method has the advantages of cheap and easily available raw materials, short reaction steps, high reaction efficiency, large preparation scale, simple preparation process and the like, has great application potential, and lays a good foundation for industrial production.