Diisopropylethylamine → (1-(5-(2-Fluorophenyl)pyrimidin-2-yl)-3-(methylsulfinyl)-1H-indol-6-yl)((S)-2-(methoxyethyl)pyrrolidin-1-yl)methanone

Participants

Reaction Steps

HATU (144 mg, 0.379 mmol, 1.5 eq) and diisopropylethylamine (0.13 mL, 0.759 mmol, 3.0 eq) were added at room temperature to a stirred solution of compound 51e) (100 mg, 0.253 mmol, 1.0 eq) and (S)-2-(methoxymethyl)pyrrolidine (0.02 mL, 0.303 mmol, 1.2 eq) in dry DMF (10 mL). The reaction mixture was stirred for 30 min and then diluted with ice water (20 mL). The precipitating solid was filtered off and dried. White solid. Yield: 110 mg (88% of theory). Melting range: 143-146° C. HPLC (method 1): Rt=10.03 min

Provenance & Evidence