3,4-dichloro-N-[1-(5-cyano-4-hydroxy-1,3-thiazol-2-yl)piperidin-4-yl]-5-methyl-1H-pyrrole-2-carboxamide → 2-(4-{[(3,4-Dichloro-5-cyano-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-carboxylic acid

Participants

Reaction Steps

The title compound was prepared by a procedure analogous to Intermediate 3 starting from methyl 2-(4-{[(3,4-dichloro-5-cyano-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-carboxylate (Example 271). The reaction mixture was concentrated to remove MeOH. Water was added and the pH was adjusted to pH 4 with NaHCO3. The product was extracted with CHCl3:isopropanol (3:1). Drying (MgSO4) and removal of solvent yielded a white solid. The was dried in drying pistol at 75° C. under vacuum.

Provenance & Evidence