Azetidine → HCID 24954113, compound

Participants

Reaction Conditions

Reaction Steps

A mixture containing 6-chloro-2-(2-chlorophenyl)-N-(5-methyl-1H-pyrazol-3-yl)pyrimidin-4-amine (430 mg, 1.34 mmol), N,N-diisopropylethylamine (1.17 ml, 6.72 mmol), azetidine (272 mL, 4.03 mmol) and n-butanol (20 mL) was heated at 108° C. overnight. The reaction mixture was cooled to room temperature and concentrated in vacuo. The concentrate was treated with ethyl acetate/Petroleum ether and water and the resulting solid filtered. The solid was washed with further quantities of ethyl acetate/Petroleum ether and water and dried in vacuo to give the title compound as a white solid (350 mg, 76%). MS (ES+) m/e=341. 1H NMR: (DMSO) 2.28-2.40 (2H, m), 3.91-4.03 (4H, m), 5.90 (1H, brs), 6.30 (1H, brs), 7.31-7.60 (4H, m), 9.28 (1H, brs), 11.88 (1H, brs).

Provenance & Evidence