Acryloyl chloride → HCID 86674085, compound

Participants

Reaction Steps

[5-(4-Amino-piperidine-1-sulfonyl)-2,3-dihydro-indol-1-yl]-cyclopropyl-methanone (0.09 g, 0.25 mmol) was dissolved in THF (5 ml). To this was added diisopropylethylamine (0.2 ml, 1.0 mmol) in one portion followed by the drop wise addition of acryloyl chloride (0.02 ml, 0.27 mmol) and the mixture was stirred at room temperature under a nitrogen atmosphere for 3 hours. After this time the mixture was diluted with EtOAc (50 ml) and washed sequentially with HCl (1M solution, 20 ml), NaOH (1M solution, 20 ml) and brine (20 ml), the organic layer was separated, dried (MgSO4), filtered and concentrated. The resulting residue was purified by flash column chromatography (elution: 100% EtOAc) to give the title compound (0.035 g, 35% yield) as a white powder.

Provenance & Evidence