A method represented by Scheme 1: wherein X represents I, Br, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents hydrogen or a negative charge; catalyst comprises a copper atom or ion, and a ligand that is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; selected from the group consisting of 2-phenylphenol, 2,6-dimethylphenol, 2-isopropylphenol, 1-naphthol, 8-hydroxyquinoline, 8-aminoquinoline, DBU, 2-(dimethylamino)ethanol, ethylene glycol, N,N-diethylsalicylamide, 2-(dimethylamino) glycine, N, N, N', N'-tetramethyl-1,2-diaminoethane, 1,10-phenanthroline, 4,7-diphenyl-1,10-phenanthroline, 4,7-dimethyl-1,10-phenanthroline, 5-methyl-1,10-phenanthroline, 5-chloro-1,10-phenanthroline, 5-nitro-1,10-phenanthroline, 4-(dimethylamino)pyridine, 2-(aminomethyl)pyridine, (methylimino)diacetic acid; cis-1,2-diaminocyclohexane, trans-1,2-diaminocyclohexane, a mixture of cis- and trans-1,2-diaminocyclohexane, cis-N, N'-dimethyl-1,2-diaminocyclohexane, trans-N, N'-dimethyl-1,2-diaminocyclohexane, a mixture of cis- and trans-N, N'-dimethyl-1,2-diaminocyclohexane, cis-N-tolyl-1,2-diaminocyclohexane, trans-N-tolyl-1,2-diaminocyclohexane, a mixture of cis- and trans-N-tolyl-1,2-diaminocyclohexane, ethanolamine, 1,2-diaminoethane, or N, N'-dimethyl-1,2-diaminoethane; base represents a carbonate or phosphate; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R' represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, heteroaryl, formyl, acyl, -CO 2 R", -C N 2, sulfonyl, -P (OR") 2, - CN, or -NO 2; wherein at least one occurrence of R' represents formyl, acyl, - CO 2 R", -C N 2, sulfonyl, -P (OR") 2, -CN, or -NO 2; R" represents independently for each occurrence optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; and C (R') 2 taken together may represent nitrile. X represents I, Br, Cl, alkylsulfonate, or arylsulfonate; Z represents optionally substituted aryl, heteroaryl or alkenyl; L represents hydrogen or a negative charge; catalyst comprises a copper atom or ion, and a ligand that is an optionally substituted aryl alcohol, alkyl amine, 1,2-diamine, 1,2-aminoalcohol, 1,2-diol, imidazolium carbene, pyridine, or 1,10-phenanthroline; selected from the group consisting of 2-phenylphenol, 2,6-dimethylphenol, 2-isopropylphenol, 1-naphthol, 8-hydroxyquinoline, 8-aminoquinoline, DBU, 2-(dimethylamino)ethanol, ethylene glycol, N,N-diethylsalicylamide, 2-(dimethylamino) glycine, N, N, N', N'-tetramethyl-1,2-diaminoethane, 1,10-phenanthroline, 4,7-diphenyl-1,10-phenanthroline, 4,7-dimethyl-1,10-phenanthroline, 5-methyl-1,10-phenanthroline, 5-chloro-1,10-phenanthroline, 5-nitro-1,10-phenanthroline, 4-(dimethylamino)pyridine, 2-(aminomethyl)pyridine, (methylimino)diacetic acid; cis-1,2-diaminocyclohexane, trans-1,2-diaminocyclohexane, a mixture of cis- and trans-1,2-diaminocyclohexane, cis-N, N'-dimethyl-1,2-diaminocyclohexane, trans-N, N'-dimethyl-1,2-diaminocyclohexane, a mixture of cis- and trans-N, N'-dimethyl-1,2-diaminocyclohexane, cis-N-tolyl-1,2-diaminocyclohexane, trans-N-tolyl-1,2-diaminocyclohexane, a mixture of cis- and trans-N-tolyl-1,2-diaminocyclohexane, ethanolamine, 1,2-diaminoethane, or N, N'-dimethyl-1,2-diaminoethane; base represents a carbonate or phosphate; R represents H, optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; R' represents independently for each occurrence H, alkyl, cycloalkyl, aralkyl, aryl, heteroaryl, formyl, acyl, -CO 2 R", -C N 2, sulfonyl, -P (OR") 2, - CN, or -NO 2; wherein at least one occurrence of R' represents formyl, acyl, - CO 2 R", -C N 2, sulfonyl, -P (OR") 2, -CN, or -NO 2; R" represents independently for each occurrence optionally substituted alkyl, cycloalkyl, aralkyl, aryl, or heteroaryl; and C (R') 2 taken together may represent nitrile.