| 摘要 |
"Process for the Aromatic Ring Acylation of 2-acyl-5-aryl-(heteroaryl)-3-hydroxycyclohex-2-en-1-ones" The invention concerns a process for the preparation of a compound of formula I wherein: the group represents an aryl group or a heteroaryl group optionally substituted with one or more electron donating groups; R1 is selected from alkyl, fluoroalkyl, alkenyl, alkynyl and phenyl; R2 is selected from hydrogen, halogen, alkyl, cyano and alkoxycarbonyl; and R3 is selected from alkyl, alkenyl, alkynyl, phenyl, substituted alkyl, substituted alkenyl, substituted alkynyl and substituted phenyl; which process comprises: reacting a compound of formula II with an acid anhydride of formula III, an acid halide of formula IV or a mixture thereof (R3CO)2O R3COhalide III IV in the presence of at least three mole equivalents, based on the compound of formula II, of anhydrous aluminium chloride. The compounds of formula I are useful intermediates for the preparation of biologically active compounds. |
