| abstract |
The present invention is aimed at providing a method for synthesizing 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene. The method is in shorter in step and more environmentally friendly, and provides a more effective synthesis strategy for the production of a key intermediate of SGLT-2 inhibitor drugs, such as Dapagliflozin, Sotagliflozin, and Ertugliflozin. The method comprises: selecting 2-chlorine-5-bromobenzoic acid and phenetole, completing a direct acylation reaction under the presence of trifluoroacetic anhydride by using boron trifluoride etherate as a catalyst, adding triethylsilane without treatment, and performing one-pot reaction to obtain a target compound, i.e., 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene. |