Process for the aromatic ring acylation of...

Details Process for the aromatic ring acylation of... Process for the aromatic ring acylation of...

C - Chemistry, Metallurgy

07

C

260/364, 260/559

C07C 45/72 (2006.01) C07C 49/835 (2006.01) C07C 65/40 (2006.01) C07C 69/716 (2006.01) C07C 69/738 (2006.01) C07D 307/46 (2006.01) C07D 307/80 (2006.01)

Patent

CA 1339277

-1- "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 Image wherein: the group Image 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 Image 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.

466547

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