IMPROVED METHODS OF ORTHO ALKYLATION

摘要

The present invention pertains to methods for preparing a compound of Formula (I), wherein A is O or N-L; each L is independently H or an acyl group; K is, together with the two contiguous linking carbon atoms, a phenyl ring, a 5- or 6-membered heteroaromatic ring or an aromatic 8-, 9- or 10-membered fused carbobicyclic or heterobicyclic ring system wherein each ring or ring system is optionally substituted; R1 is H, C1 to C4 alkyl or CO2R3; R2 is H or C1 to C4 alkyl; and R3 is C1 to C4 alkyl; comprising hydrogenating a compound of Formula (II), wherein n is 0, 1 or 2 in the presence of a catalyst comprising palladium to form the compound of Formula (I). This invention further pertains to methods for preparing compounds of Formula (II) useful for preparing compounds of Formula (I). This invention also pertains to compounds used in these methods.