| 主权项 |
1. A process for preparing a 3,5-disubstituted 1,2,4-oxadiazole of Formula (Ia), or a salt thereof, the process comprising reacting an N-hydroxyamidine of Formula (IIa), or a tautomeric form thereof, with an acyl chloride of Formula (IIIa), in a reaction mixture comprising an organic phase and an aqueous phase, wherein the reaction mixture comprises a water-immiscible organic solvent and an aqueous base, wherein the temperature of the reaction mixture is no greater than about 85° C.; wherein Ar1 is selected from the group consisting of phenyl, pyridyl, pyrazyl, oxazolyl or isoxazolyl, each of which can be optionally independently substituted with one or more substituents selected from the group consisting of halogen, CF3, CH3, OCF3, OCH3, CN and C(H)O; and Ar2 is thienyl, which can be optionally independently substituted with one or more substituents selected from the group consisting of fluorine, chlorine, CH3, and OCF3; and wherein the acyl chloride of Formula (III) is prepared from 2-thiophenecarboxylic acid. |
