The invention relates to an ortho-position dihalogen substitution compound of
aryl pyrimidine and a preparing method thereof. The compound has the following
structural formula I: R1=H, p-Me, p-Cl, p-COOEt, p-CF3, m-Me, m-OMe, R2=H, 4-Ph, 5-Ph, X=Cl, Br. The invention comprises the following steps: dissolving
aryl pyrimidine,
palladium acetate, additive and
halogenation calcium into
acetic acid, stirring, and reacting until reaction
raw material disappears; removing
solvent, adding saturation
sodium bicarbonate solution into a
system, and extracting a product with
ethyl acetate; obtaining a crude product by
drying the organic phase and removing the
solvent; purifying the product to obtain the corresponding ortho-position dihalogen substitution compound of
aryl pyrimidine. The compound of the invention is a kind of important
organic synthesis intermediate. The invention has easily obtained
raw material, high reaction selectivity, and adopts
calcium chloride and
calcium bromide with low price as a
halogen source, uses common
solvent in reaction, and has simple operation, moderate reaction condition and
environmentally friendly reaction, maximum reaction yield can reach 95%, so that the invention is very suitable for industrial production.