Triethylamine → HCID 60052341, compound

Participants

Reaction Conditions

Reaction Steps

Dissolve (R)-1-(5-bromo-pyridin-2-yl)-pyrrolidin-3-ol (6.8 g, 27.64 mmol), (prepare according to Stenkamp, D. et al WO 2005103032) in CH2Cl2 (50 mL), and cool to 0° C. Treat the mixture with Et3N (5.0 mL, 35.93 mmol), followed by MsCl (2.4 mL, 30.4 mmol). Stir the mixture at 0° C. for 30 min and then at RT for 1 h. Dilute with CH2Cl2 (100 mL), and wash with H2O (100 mL), and brine (100 mL). Dry with Na2SO4, filter, and concentrate. Purify the crude material by chromatography, eluting with 50-70% EtOAc/hexane, to give 8.86 g (97%) of the title compound. MS/ES m/z (79Br) 321.0 [M+H]+.

Provenance & Evidence