The invention discloses a method for synthesizing a five-membered
lactam skeleton
bulk drug with high optical purity under the
catalysis of
rhodium, which is characterized in that racemic and cheap gamma-substituted alpha, beta-unsaturated gamma-
lactam is used as a
raw material, a dicyclooctene hydroxyl
rhodium (I)
dimer is used as a catalyst, a cheap chiral
phosphine ligand is used as a ligand, and the
raw material is synthesized by a one-
step method. The high enantioselectivity arylation reaction with arylboronic acid is realized. According to the method, the optical purity limit of a traditional
route is successfully broken through, the
specific rotation of the obtained trans-beta, gamma-disubstituted gamma-lactams with three single configurations is remarkably higher than the highest value in the literature, and a high-enantioselectivity key synthesis building block is provided for synthesis of a
protein kinase C
regulator, a
glutamate receptor antagonist and CGN-10100. The method provided by the invention is simple and easy to operate, mild in reaction condition, high in yield and strong in derivation ability, and provides a new method for efficient and high-enantioselectivity preparation of chiral bulk drugs.