Patent ID: 7214768

Claim:
A process for preparing Compound 5A of the structure while minimizing the formation of Compounds 5B and Compound 5C of the structure or their pharmaceutically acceptable salts, hydrates or solvates thereof, which comprises the steps of: A) reacting Compound 4 of the structure wherein R is C(═O)NH 2 , CH 2 NH 3 +X— or CN; X—is Cl − , CF 3 COO − , CH 3 COO − , CF 3 SO 3 − , HSO 4 − ; and R 3 is aryl, wherein aryl is defined as phenyl or naphthyl, substituted or unsubstituted with C 1 –C 6 -alkyl, C 1 –C 6 -alkoxy, halo (Br, Cl, F, I), (CH 2 )aryl, heteroaryl, wherein heteroaryl is defined as 5-membered ring, 6-membered ring, 5,6-fused ring, or 6,6-fused ring bearing 1 to 3 heteroatoms selected from N, O, or S optionally substituted with C 1 –C 6 -alkyl, or C 1 –C 6 -alkoxy; with a boronic acid or borate in a solvent to afford boronate(s) or borate(s), respectively, of compound 4; and B) reacting the boronate or borate with a thiol, R 3 SH, wherein R 3 is as defined above, and an acid in the amount of 1 eq. of the thiol R 3 SH to afford Compound 5A with minimal amounts of Compounds 5B and 5C.