Hydrogen Peroxide → HCID 42636084, compound

Participants

Reaction Steps

To a stirred solution of 7-(2-aminopyrimidin-5-yl)-{[(1R)-1-cyclopropyl-2,2,2-trifluoroethyl]amino}-8-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-5H-pyrido[4,3-b]indole-4-carboxamide (218 mg, 0.38 mmol) in AcOH (7.7 mL) was added hydrogen peroxide (30%, 0.20 mL, 1.9 mmol) at 0° C. The reaction was left to stir at room temperature for 3 h, diluted with EtOAc, and washed with water. The organic layer was dried, concentrated, and purified by flash chromatography to afford the title compound. 1H NMR (500 MHz, CD3SOCD3) δ 11.38 (s, 1H); 9.25 (s, 1H); 8.42 (s, 2H); 7.97 (s, 1H); 7.90 (br s, 1H); 7.75 (s, 1H); 7.60 (s, 1H); 7.22 (br s, 1H); 6.63 (m, 2H); 4.86 (m, 1H); 1.45 (m, 1H); 0.72 (m, 1H); 0.60 (m, 1H); 0.53 (m, 1H); 0.36 (m, 1H). LRMS (APCI) calc'd for (C21H18F3N7O2) [M+H]+, 458.1. found 458.1.

Provenance & Evidence