Triethylamine → HCID 58042856, compound

Participants

Reaction Steps

To 45 mg (0.13 mmol) 1-[2-(4-hydroxymethyl-phenyl)-ethyl]-4-(pyridin-4-ylmethoxy)-1H-pyridin-2-one (example 10.1a) in 3.0 mL DCM is added at RT 56 μL (0.40 mmol) triethylamine and subsequently 21 μL (0.27 mmol) methanesulfonyl chloride. The reaction mixture is stirred 1 h at RT. Additional 56 μL triethylamine (0.40 mmol) and subsequently 21 μL (0.27 mmol) methanesulfonyl chloride are added at RT and the reaction mixture is stirred for additional 1.5 h. Then 22 μL (0.27 mmol) pyrrolidine is added. The mixture is stirred overnight at RT, diluted with 50 mL DCM and is washed four times with water. The organic phase is dried over MgSO4, filtered and the solvent is evaporated. The residue is purified via chromatography (silica gel; DCM/MeOH/NH4OH 9:1:0.1 to 8:2:0.2).

Provenance & Evidence