| abstract |
The invention discloses a process for synthesizing ezetimibe, belonging to the technical field of pharmaceutical synthesis. Compound I is used as a starting material, and intermediate I is obtained through hydroxyl protection, and intermediate I and compound II are subjected to 1,4 addition reaction to obtain Intermediate II, the intermediate II is then subjected to enzymatic chiral reduction to obtain the ezetimibe finished product; the enzymatic reaction of the present invention is designed in seconds, and under the action of a specific chiral enzyme, the carbonyl group of the intermediate II is bound to the activity of the enzyme. The center position, and forcibly freezes the translation and rotation of the chemical bond of the reactant target, prompting the reaction to react in the correct direction, which is conducive to the formation of chiral bonds. |