Patent ID: 7232923

Claim:
A process for forming a compound of formula I comprising reacting a compound of formula II with a compound of formula III in the presence of the catalyst [(R-BINAP)Pd(solvent) 2 ] 2+ [TfO] − 2 wherein R 1 is selected from the group consisting of: (a) a peptide, an amino acid, a dipeptide, a sugar, and a polymer; and (b) H, C 1-12 alkyl, C 2-12 alkenyl, C 2-12 alkynyl C 3-12 aryl and C 3-12 heterocyclyl; which is optionally substituted by one or more of C 1-6 alkyl, halogen, C 1-6 haloalkyl, OR 5 , SR 5 , NO 2 , CN, NR 5 R 5 , NR 5 COR 5 , NR 5 CONR 5 R 5 , NR 5 COR 5 , NR 5 CO 2 R 5 , CO 2 R 5 , COR 5 , CONR 52 , S(O) 2 R 5 , SONR 52 , S(O)R 5 , SO 2 NR 5 R 5 , NR 5 S(O) 2 R 5 ; wherein each R 5 is individually selected from hydrogen, C 1-6 alkyl, C 1-6 haloalkyl and C 6-12 aryl; R 2 is hydrogen, C 1-12 alkyl, or aryl or with the adjacent carboxyl group forms an amino protecting group such as a carbamate including benzyloxycarbonyl, t-butoxycarbonyl, 2-(4-biphenylyl)-isopropoxycarbonyl, 9-fluorenylmethoxycarbonyl, wherein said alkyl or aryl group can be optionally substituted with one or more of those groups selected from C 1-6 alkyl, halogen, C 1-6 haloalkyl, OR 5 , SR 5 , NO 2 , CN, NR 5 R 5 , NR 5 COR 5 , NR 5 CONR 5 R 5 , NR 5 COR 5 , NR 5 CO 2 R 5 , CO 2 R 5 , COR 5 , CONR 52 , S(O) 2 R 5 , SONR 52 , S(O)R 5 , SO 2 NR 5 R 5 , NR 5 S(O) 2 R 5 , wherein the C 1-12 alkyl group optionally incorporates one or two insertions selected from the group consisting of —O—, —N(R 5 )—, —S(O)—and —S(O 2 )—, wherein each R 5 is the same or different; R 3 is H or C 1-12 alkyl; R 4 is aryl or heterocycyl, wherein the aryl or heteroaryl group is optionally substituted with one or more of the groups described for R 2 ; and R 5 is hydrogen, C 1-6 alkyl, C 1-6 haloalkyl or C 6-12 aryl.