The invention discloses a method for synthesizing a
camptothecin chiral precursor with high enantioselectivity, and belongs to the field of
organic synthesis. In the invention, the preparation of a chiral precursor
amide compound of
camptothecin comprises the following steps: synthesizing corresponding
aryl (E)-2-ethylbutyl-2-olefine acid ester, mixing the
aryl (E)-2-ethylbutyl-2-olefine acid ester with a
phase transfer catalyst derived from cinchona
alkaloid in an
organic solvent, sequentially adding acid,
potassium permanganate and a small amount of
potassium fluoride solution for reaction, and after the reaction is finished, performing suction
filtration to obtain the chiral precursor
amide compound of
camptothecin. Carrying out amine ester exchange with
diethylamine; and evaporating the
solvent, and quickly purifying by using a
silica gel column to obtain the camptothecin precursor chiral
amide compound with high enantioselectivity. The invention aims at providing a new thought and a new method for
total synthesis of camptothecin based on a camptothecin chiral precursor reported in literatures, and broadens a synthesis
route for synthesizing camptothecin.