Azetidine → HCID 69093675, compound

Participants

Reaction Steps

A solution of 2-(5-bromo-1-(2-fluorobenzyl)-1H-1,2,4-triazol-3-yl)pyridine (I-16), in DMA was treated with a large excess of azetidine (˜30 eq). The resultant solution was warmed to 100° C. and stirred at that temperature for 18 h. The reaction solution was cooled to rt, poured into 1N NaOH solution and then extracted with EtOAc. The organic phases were dried over Na2SO4, filtered and conc. The crude product was purified using SiO2 chromatography and an appropriate gradient (MeOH—CH3CN (1:7)/CH2Cl2) to give 2-(5-(azetidin-1-yl)-1-(2-fluorobenzyl)-1H-1,2,4-triazol-3-yl)pyridine, I-23, as a white solid (88% yield).

Provenance & Evidence