Abstract: A chiral bimetallic cooperative catalysis system and use thereof in asymmetric synthesis of bedaquiline are provided. Specifically, the chiral bimetallic cooperative catalysis system is formed by a metallic lithium, sodium or potassium salt and another metal salt under the action of a suitable ligand and an additive. By means of the chiral bimetallic cooperative catalysis system, an addition reaction of 6-bromo-3-benzyl-2-methoxyquinoline (I) and 3-dimethylamino-1-naphthyl-1-propanone (II) is promoted, the selectivity is regulated, and a target product, (1R,2S)-bedaquiline, with high yield and high selectivity is obtained for the first time.

Abstract: A method for catalytic asymmetric synthesis of a phosphorus-stereogenic (P-stereogenic) nucleoside derivative of formula (3) and a catalyst used therein. The P-stereogenic nucleoside derivative (3) can be hydrolyzed to obtain remdesivir.

Abstract: A method for catalytic asymmetric synthesis of a phosphorus-stereogenic (P-stereogenic) nucleoside derivative of formula (3) and a catalyst used therein. The P-stereogenic nucleoside derivative (3) can be hydrolyzed to obtain remdesivir. Specifically, a nucleoside and phosphoryl chloride are subjected to asymmetric reaction under the catalysis of a chiral bicyclic imidazole catalyst in the presence of a base to produce the P-stereogenic nucleoside derivative.