Cesium carbonate → HCID 59618055, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of N-(2-bromopyridin-4-yl)-2,4,6-trichlorobenzamide (76 mg, 0.20 mmol), pyrimidin-4-amine (38 mg, 0.40 mmol), Pd2(dba)3 (18.3 mg, 0.020 mmol), Xantphos (23.3 mg, 0.040 mmol), Cs2CO3 (131 mg, 0.40 mmol), and dioxane (1.2 mL) was heated at 140° C. for 1 hour in a microwave reactor under nitrogen atmosphere. The mixture was filtered through Celite and concentrated under reduced pressure. The residue was purified by prep-HPLC (Gilson GX 281, Shim-pack PRC-ODS 250 mm×20 mm×2, gradient: CH3CN/10 mm/L NH4HCO3, 17 min) to afford the desired product (46.5 mg, yield: 59%). 1H NMR (500 MHz, MeOH-d4): δ 8.68 (s, 1H), 8.36 (d, J=6.0 Hz, 1H), 8.26 (d, J=6.0 Hz, 1H), 8.19 (s, 1H), 7.71 (d, J=6.0 Hz, 1H), 7.65 (s, 2H), 7.35 (m, 1H). LCMS (ESI) m/z: 394.0 [M+H+].

Provenance & Evidence