The invention discloses an alpha-fluoro alpha, beta-unsaturated
amide derivative as well as a synthesis method and application thereof. The preparation method comprises the following steps: by taking amyl-1, 1, 2-trifluoro-1, 4-
diene which is simple and convenient to prepare and a cheap and abundant amine compound as raw materials, an allyl
palladium chloride dimer as a
transition metal catalyst, 1, 4-bis (
diphenylphosphine)
butane as a ligand and 2, 5-di-tert-butylbenzoquinone as an oxidant, reacting in an
organic solvent at a proper temperature under a
nitrogen condition, thereby obtaining the 1, 1, 2-trifluoro-1, 4-
diene compound. The alpha-fluoro alpha, beta-unsaturated
amide derivative is obtained with good yield, and the
structural formula of the derivative is shown in the specification. The synthesis method disclosed by the invention has the characteristics of simplicity and convenience in operation, mild conditions, greenness, economy, wide substrate compatibility, high chemical selectivity and high
regioselectivity, and solves the technical problem that the synthesis conditions of the alpha-fluoro-alpha, beta-unsaturated
amide derivative are complicated and harsh. Meanwhile, the alpha-fluoro
drug molecules can be efficiently and highly selectively obtained, and the method has a wide application prospect.