abstract |
The object of the present invention is to provide a method for the synthesis of 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene with a shorter step and greener steps, which are dapagliflozin, soxagliflozin The production of key intermediates for SGLT-2 inhibitor drugs such as ipagliflozin and epagliflozin provides more efficient synthetic strategies. Selecting 2-chloro-5-bromobenzoic acid and phenethyl ether, in the presence of trifluoroacetic anhydride, using boron trifluoride diethyl ether as a catalyst to complete the direct acylation reaction, without treatment, adding triethylsilane for one-pot reaction to obtain The target compound is 4-bromo-2-(4'-ethoxy-benzyl)-1-chlorobenzene. |