A process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent selected from the group consisting of 2-chloro-1,3-dimethyl-2-imidazolium tetrafluoroborate, HBTU, HCTU, 2-chloro-4,6-dimethoxy-1,3,5-triazine, HATU, HOBT/EDC, and propane phosphonic anyhdride; wherein each R 2 and R 4 is independently selected from hydrogen, CN, CF 3, halo, C 1-6 straight or branched alkyl, 3-12 membered cycloaliphatic, phenyl, C 5-10 heteroaryl or C 3-7 heterocyclic, wherein said heteroaryl or heterocyclic has up to 3 heteroatoms selected from O, S, or N, and each C 1-6 straight or branched alkyl, 3-12 membered cycloaliphatic, phenyl, C 5-10 heteroaryl or C 3-7 heterocyclic is independently and optionally substituted with up to three substituents selected from -OR', -CF 3, -OCF 3, SR', S R', SO 2 R', -SCF 3, halo, CN, -COOR', -COR'-, -O(CH 2) 2 N(R')(R'), -O(CH 2)N(R')(R'), - CON(R')(R'), -(CH 2) 2 OR', -(CH 2)OR', CH 2 CN, optionally substituted phenyl or phenoxy, -N(R')(R'), - NR'C OR', -NR'C R', -(CH 2) 2 N(R')(R'), or -(CH 2)N(R')(R'); R 5 is -OC OR', -OC NHR', -OC NR' 2, wherein R' is not hydrogen, or R 4 and R 5 taken together form the moiety each X is independently a bond or is an optionally substituted C 1-6 alkylidene chain wherein up to two methylene units of X are optionally and independently replaced by -CO-, -CS-, -COCO-, -CONR'-, -CONR'NR'-, -CO 2 -, -OCO-, -NR'CO 2 -, -O-, -NR'CONR'-, -OCONR'-, -NR'NR', -NR'NR'CO-, -NR'CO-, -S-, -SO, -SO 2 -, -NR'-, -SO 2 NR'-, NR'SO 2 -, or -NR'SO 2 NR'-; each R X is independently R', halo, NO 2, CN, CF 3, or OCF 3; y is an integer from 0-4; and each R' is independently selected from hydrogen or an optionally substituted group selected from a C 1-8 aliphatic group, a 3-8-membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two occurrences of R' are taken together with the atom(s) to which they are bound to form an optionally substituted 3-12 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from N, O, or S. each R 2 and R 4 is independently selected from hydrogen, CN, CF 3, halo, C 1-6 straight or branched alkyl, 3-12 membered cycloaliphatic, phenyl, C 5-10 heteroaryl or C 3-7 heterocyclic, wherein said heteroaryl or heterocyclic has up to 3 heteroatoms selected from O, S, or N, and each C 1-6 straight or branched alkyl, 3-12 membered cycloaliphatic, phenyl, C 5-10 heteroaryl or C 3-7 heterocyclic is independently and optionally substituted with up to three substituents selected from -OR', -CF 3, -OCF 3, SR', S R', SO 2 R', -SCF 3, halo, CN, -COOR', -COR'-, -O(CH 2) 2 N(R')(R'), -O(CH 2)N(R')(R'), - CON(R')(R'), -(CH 2) 2 OR', -(CH 2)OR', CH 2 CN, optionally substituted phenyl or phenoxy, -N(R')(R'), - NR'C OR', -NR'C R', -(CH 2) 2 N(R')(R'), or -(CH 2)N(R')(R'); R 5 is -OC OR', -OC NHR', -OC NR' 2, wherein R' is not hydrogen, or R 4 and R 5 taken together form the moiety each X is independently a bond or is an optionally substituted C 1-6 alkylidene chain wherein up to two methylene units of X are optionally and independently replaced by -CO-, -CS-, -COCO-, -CONR'-, -CONR'NR'-, -CO 2 -, -OCO-, -NR'CO 2 -, -O-, -NR'CONR'-, -OCONR'-, -NR'NR', -NR'NR'CO-, -NR'CO-, -S-, -SO, -SO 2 -, -NR'-, -SO 2 NR'-, NR'SO 2 -, or -NR'SO 2 NR'-; each R X is independently R', halo, NO 2, CN, CF 3, or OCF 3; y is an integer from 0-4; and each R' is independently selected from hydrogen or an optionally substituted group selected from a C 1-8 aliphatic group, a 3-8-membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two occurrences of R' are taken together with the atom(s) to which they are bound to form an optionally substituted 3-12 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from N, O, or S.