DCC Mediated Coupling for Halofenate Manufacture

摘要

The present application discloses a process for the preparation of a halofenate compound of the formula (III) or a salt thereof:;;wherein R, X and X′ are as defined herein, the process comprising contacting a compound of formula (Ia) with a compound of formula (Ib) and N,N′-dicyclohexylcarbodiimide under conditions sufficient to form the compound of formula (III).

主权项

1. A process for the preparation of a compound of formula (III) or a salt thereof:wherein:
R is selected from the group consisting of arylC1-6alkyl-, (C1-6alkyl)2NC1-6alkyl-, C1-6alkyl-NHC1-6alkyl-, C1-6alkylC(O)NHC1-6alkyl-, arylC(O)NHC1-6alkyl-, C1-6alkyl-NHC(O)NHC1-6alkyl-, aryloxyC1-6alkyl- and C1-6alkylNHC(O)NHphenyl-; and X and X′ are each independently a halogen; the process comprising: contacting a compound of the formula (Ia) wherein X and X′ are each independently a halogen; with a compound of formula (Ib)
ROH  (Ib) and a coupling agent; in an aprotic solvent under conditions sufficient to form the compound of formula (III).