Dimethylacetamide → HCID 178493096, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 5,6-dichloro-N2-[(1S)-1-(5-fluoropyrimidin-2-yl)ethyl]-N4-(5-methoxy-1H-pyrazol-3-yl)pyrimidine-2,4-diamine (Example 30, 100 mg), zinc (17 mg), zinc cyanide (31 mg), DPPF (7 mg) and Pd2(dba)3 (12 mg) in DMA (2.0 ml) was degassed and heated at 100° C. for 2 hours. The solution was separated between ethyl acetate and water. Organic 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 (42.5 mg). 1H NMR δ 10.20 (s, 1H) 8.89 (s, 2H) 8.56 (bs, 1H) 5.63 (s, 1H) 5.03-5.29 (m, 1H) 3.75 (s, 3H) 1.47 (d, 3H); m/z 390.

Provenance & Evidence