Cesium carbonate → Methyl 3-amino-6-{[2-(4-chlorophenyl)-1,3-oxazol-4-yl]methoxy}-5-cyano-4-[4-(2-hydroxyethoxy)phenyl]-1-methyl-1H-pyrrolo[2,3-b]pyridine-2-carboxylate

Participants

Reaction Conditions

Reaction Steps

20 mg (0.04 mmol) of the compound from Example 51A were initially charged in 1 ml of acetonitrile, and 45 mg (0.14 mmol) of cesium carbonate were added. The reaction mixture was stirred at 50° C. for 4 h. After cooling to RT, the mixture was filtered off. The precipitate was washed with acetonitrile and suspended in water. The mixture was extracted three times with in each case 10 ml of ethyl acetate, and the combined organic phases were dried over magnesium sulfate. After removal of the solvent on a rotary evaporator, the residue was purified directly by preparative HPLC (column: YMC GEL ODS-AQ S-5/15 μm; mobile phase gradient: acetonitrile/water 10:90→95:5). Removal of the solvent on a rotary evaporator gave the product as a solid.

Provenance & Evidence