The invention discloses a method for compounding a trans-hydroxyl
active metabolite of
loxoprofen. The method comprises the following steps: taking 2-[p(bromomethyl)phenyl]propionic acid as a
raw material and carrying out resolution and methyl esterification, thus obtaining an intermediate, namely, a compound as shown in a formula 3; preparing a chiral assistant, namely, a compound as shown in a formula 7, by starting from L-phenylalaninol; firstly forming
Schiff base as shown in a formula 9 by
cyclopentanone and the chiral assistant, namely, the compound as shown in the formula 7, and then condensing the
Schiff base as shown in the formula 9 and the intermediate, namely, the compound as shown in the formula 3, into an intermediate, namely, a compound as shown in a formula 11; carrying out acidic
hydrolysis on the intermediate, namely, the compound as shown in the formula 11, and perfroming stereoselective reduction on
cyclopentanone carbonyl groups, thus obtaining the trans-hydroxyl
active metabolite, namely, a compound as shown in a formula TM. In a compounding path, raw materials can be easily obtained, the operation is convenient, environmental friendliness is realized, a separation means of
column chromatography is prevented from being used, and the technical requirements of industrial large-scale production can be completely met.