Provided are a method for preparing (R)-
ketorolac and use thereof, belonging to the technical field of
organic synthesis. The method includes the following steps: step 1, preparing
ketorolac; and step 2, subjecting the
ketorolac to resolution to obtain the (R)-ketorolac, the resolution being selected from the group consisting of
chiral amine resolution and
enzyme resolution. In the disclosure, glacial
acetic acid is used as a reaction
solvent, which is not only clean and environmental-friendly, but also easy to be removed. The glacial
acetic acid could significantly improve a conversion rate of SM1 as a
raw material, thereby improving the yield and the purity of the ketorolac, such that the ketorolac has a yield of not less than 70% and a purity of not less than 99%. The ketorolac is subjected to
chiral resolution by the
chiral amine or the
enzyme to obtain the (R)-ketorolac with a high purity and a high yield, and the (R)-ketorolac could prevent
chemotherapy resistance and improve both chemotherapeutic
efficacy and
cure rate.