The invention discloses a preparation method of fiazonetin, and belongs to the technical field of
medicinal chemistry. According to the
route, 2-halo-3-methylpyrazine which is low in price and easy to obtain is used as a
raw material and sequentially reacts with hydrazine
hydrate and
orthoester, and then a hydrogenation reduction reaction is performed to generate a compound 4; carrying out
chiral resolution or chiral separation on the compound 4 and carrying out
condensation reaction on the compound 4 and p-fluorobenzoyl
halide to obtain an intermediate compound 5 or 5'and a new intermediate compound 6; reacting the compound 6 with a halogenating
reagent to obtain a compound 7; carrying out Suzuki
coupling reaction on the compound 7 and a compound 8 to obtain a compound, namely, the compound of the formula A, namely, non-azonepan; according to the
route, the raw materials are simple, easy to obtain and low in cost; the reaction is simple, the preparation efficiency is high, and the reaction yield of each step can be higher than 90%; no harsh
reaction conditions exist, and operation is safe; post-treatment is simple and convenient, and environmental
pollution is low. The method is suitable for large-scale production; a high-chiral product can be obtained, the chiral purity value of a final product is as high as 99.5%, and the method has relatively good market value and profound practical significance. # imgabs0 #