Water → HCID 178428419, compound

Participants

Reaction Steps

A solution of 375 mg (1.09 mmol) 2-methyl-4-(3-methyl-1H-indazol-5-yl)-6-(trifluoromethyl)-1,4-dihydropyridine-3,5-dicarbonitrile (Example 4) in DMF (11.5 ml) was cooled to 0° C. 534 mg (1.64 mmol) caesium carbonate were added at this temperature, and after 15 min 48 μl (0.77 mmol) methyl iodide were added dropwise at room temperature. After stirring overnight at rt, additional methyl iodide (20 μl) and a small amount of caesium carbonate were added, and the reaction mixture was stirred at rt for further 3 h before water and methanol were added. The resulting solution was directly purified by preparative RP-HPLC (acetonitrile/water+0.1% TFA gradient) to give 75 mg (19% of th.) of the racemic title compound.

Provenance & Evidence