| abstract |
The present invention belongs to the field of pharmaceutical preparation, and relates to a novel process for the preparation of substituted phenylacetic acid derivatives, in particular to the preparation of 2-(4-(2-oxocyclopentyl)phenyl)propanoic acid. A method for preparing loxopropene in a precursor form using a 1,4-di-halobenzyl compound or a disubstituted benzyl compound as a starting material is achieved through a substitution reaction of a cyclopentanone group or a precursor compound thereof. wherein X is halogen and L 1 is a suitable leaving group selected from halogen, OH, OMs, OTs, OTf and the like; L 2 is selected from halogen, CN, OH, -CH 2 OH, -CHO, CH 3 NO 2 , ester group, -NR 4 R 5 , OTf, OTs, OMs, -C=CR 6 , -C≡CR 7 , etc. suitable leaving groups are wherein R 4 , R 5 , R 6 , R 7 are short chain alkyl groups; Z is a cyclopentanone group selected from et al. and its precursor form; R 3 is a short chain alkyl group; L 3 is a suitable leaving group selected from halogen, OH, OMs, OTs, OTf, etc., or an organometallic group. The present invention also includes a detailed procedure for converting the precursor compound of cyclopentanone group to cyclopentanone, and then converting the precursor compound of loxopropene to loxopropene. |