2-Bromoethanol → HCID 118364830, compound

Participants

Reaction Steps

(S)-2-fluoro-5-(1-((4-(5-(1,2,3,6-tetrahydropyridin-4-yl)pyrimidin-2-yl)morpholine-2-yl)methyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)benzonitrile 44 mg (0.09 mmol) was dissolved in DMF 1 ml. Potassium carbonate 36 mg (0.26 mmol) and 2-bromoethanol 0.009 ml (0.13 mmol) were added, and Et3N (2 drop) were added, followed by stirring at room temperature for 13 hours under nitrogen gas. When the reaction was completed, the reaction mixture was extracted two times or more with ethyl acetate and water, and concentrated under reduced pressure. PCL using 10% dichloromethane/methanol gave (S)-2-fluoro-5-(1-((4-(5-(1-(2-hydroxyethyl)-1,2,3,6-tetrahydropyridin-4-yl)pyrimidin-2-yl)morpholin-2-yl)methyl)-1H-[1,2,3]triazolo[4,5-b]pyrazin-6-yl)benzonitrile 9 mg (0.017 mmol) with a yield of 19%.

Provenance & Evidence