| abstract |
The present invention relates to the technical field of biopharmaceuticals, in particular to the preparation of sofosbuvir intermediates, more specifically to sofosbuvir intermediates ((2R, 3R, 4R)-3-benzoyloxy-4 -Fluorine-5-chloro-4-methyltetrahydrofuran-2-yl) the preparation method of methyl benzoate, make the compound shown in formula b after the compound shown in formula a reacts with modified red aluminum, then make The compound represented by formula b undergoes chlorination reaction in oxalyl chloride/chlorobenzene solution to obtain the compound represented by formula c, and finally the compound represented by formula c is reacted with the compound of formula e to obtain the target compound represented by formula d. The reaction conditions of the preparation process of the invention are simple and easy to operate, and the cost is low; in the post-treatment process of the chlorination stage, the operation of hydrolysis is reduced, the amount of waste water is reduced, and the environment is more friendly; the preparation process of the invention has high yield and product High purity, more stable product, suitable for mass production. |