Triethylamine → 2-(5-Bromopyridin-3-yl)-2-azabicyclo[3.1.0]hex-3-ylmethyl methanesulfonate

To an ice-cold solution of [2-(5-Bromopyridin-3-yl)-2-azabicyclo[3.1.0]hex-3-yl]methanol (462 mg, 2.43 mmol) in dry dichloromethane (10 mL) was added triethylamine (0.51 mL, 3.6 mmol) followed by methanesulfonyl chloride (334 mg, 2.92 mmol). The reaction mixture was gradually warmed to room temperature and stirred for 1 hour. The volatiles were removed under reduced pressure and the crude product was purified by flash column chromatography to obtain title compound of 586 mg as gummy liquid. Yield: 90%.

1. customThe volatiles were removed under reduced pressure
2. customthe crude product was purified by flash column chromatography

ORD-Eintrag

ord-3ba3678bc5f94c3eba5e6deaa328a185

Quelldatensatz

uspto-grants-2014_02

DOI

10.6084/m9.figshare.5104873.v1

Patentnummer

US08653071B2