Water → 2-(4-{[(3,4-Dichloro-5-methyl-1H-pyrrol-2-yl)carbonyl]amino}piperidin-1-yl)-1,3-thiazole-5-sulfonic acid

Participants

Reaction Conditions

Reaction Steps

3,4-Dichloro-5-methyl-N-[1-(1,3-thiazol-2-yl)piperidin-4-yl]-1H-pyrrole-2-carboxamide (Example 329; 692 mg, 1.93 mmol) was dissolved in anhydrous DCM. Chlorosulfonic acid (513 μl, 7.7 mmol) was added slowly and the mixture was heated at 60° C. for 2 h. The mixture was cooled to 0° C. and water was added, whereupon a brown solid separated. This was filtered and washed well with water, dried in vacuo to give the title compound (393 mg).

Provenance & Evidence