Triethylamine → (3S)-1-(5-Bromopyridin-2-yl)pyrrolidin-3-ol

Participants

Reaction Steps

Heat 5-bromo-2-fluoro-pyridine (10.33 g, 57.39 mmmol) in THF (50 mL) with (S)-3-hydroxypyrrolidine (5.00 g, 57.39 mmol) and Et3N (9.2 mL, 68.87 mmol) in a microwave reactor at 120° C. for 45 min. Dilute with EtOAc (150 mL), and wash with saturated NaHCO3 (2×50 mL) and water (100 mL). Dry with Na2SO4, filter, and concentrate. Purify the crude material by chromatography, eluting with 100% EtOAc to give 10.13 g (72%) of the title compound. MS/ES m/z (79Br) 244.0 [M+H]+.

Provenance & Evidence