Triethylamine → HCID 25121261, compound

Participants

Reaction Conditions

Reaction Steps

Slowly add methanesulfonyl chloride (0.04 mL, 0.55 mmol) to a solution of newly synthesized 1-(4-(2-(2-(2-(1H-1,2,3-triazol-1-yl)ethylamino)-5-fluoropyrimidin-4-yl)benzo[b]thiophen-7-yl)-6-fluoropyridin-3-yl)ethanol (240 mg, 0.50 mmol) and triethylamine (0.14 mL, 1.0 mmol) in methylene chloride (5 mL) at −78° C. After stirring the mixture at the same temperature for another 60 min, add cyclopropylamine (0.040 mL, 0.55 mmol) and leave it overnight at RT. Heat it to 45° C. for 5 h, cool to RT, and remove the solvent. Purify by column chromatography (10% methanol in DCM) to afford the title compound (42 mg 17%). MS (ES) m/z 519 [M+1]+.

Provenance & Evidence