Diisopropylethylamine → 5-Chloro-N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]pyrimidine-2,4-diamine

Participants

Reaction Conditions

Reaction Steps

A mixture of (S)-1-(5-fluoropyrimidin-2-yl)ethanamine hydrochloride (Method 7, 93 mg), 2,5-dichloro-N-(5-cyclopropyl-1H-pyrazol-3-yl)pyrimidin-4-amine (Method 15, 135 mg) and DIPEA (0.26 ml) in n-BuOH (2.5 ml) was charged into a microwave reaction vessel. The vessel was sealed and heated in microwave reactor at 180° C. for 6 hours. The solvent was removed under reduced pressure and the residue was purified by Gilson (10-50% MeCN/H2O, 15 minutes) to give the titled compound as solid (435 mg). NMR: 10.64 (s, 1H), 8.91 (s, 3H), 8.30 (s, 1H), 5.97 (s, 1H), 5.17 (s, 1H), 1.83-1.97 (m, 1H), 1.56 (d, 3H), 0.93-1.09 (m, 2H), 0.63-0.77 (m, 2H). m/z 413.

Provenance & Evidence