The invention discloses a synthesis process of
dapagliflozin. The method comprises the following steps: (1) preparing a
Grignard reagent THF solution of 1-chloro-2-(4-ethoxybenzyl)-4
iodobenzene; (2) preparing 2, 3, 4, 6-
tetra-O-acetyl-alpha-D-glucopyranosyl
bromide; (3) in the presence of a catalyst containing
anhydrous cerium chloride and
titanium tetraisopropoxide, carrying out coupled reaction on the
Grignard reagent THF solution obtained in the step (1) and the 2, 3, 4, 6-
tetra-O-acetyl-alpha-D-glucopyranose
bromide obtained in the step (2) at the temperature of-15 to-10 DEG C to obtain an acetylated
dapagliflozin intermediate; and (4) carrying out deprotection reaction on the acetylated
dapagliflozin intermediate obtained in the step (3) to obtain the dapagliflozin. Under a composite catalytic
system, the reaction shows excellent
stereoselectivity, the required beta-configuration C-
glycoside product is specifically generated, and the generation of by-products such as alpha-isomers and the like is effectively inhibited.