Potassium Phosphate, Tribasic → 1-{[(1R,2R,4R)-4-Hydroxy-2-methylcyclohexyl]amino}-7-(1-methyl-1H-pyrazol-4-yl)-5H-pyrido[4,3-b]indole-4-carbonitrile

Participants

Reaction Conditions

Reaction Steps

A flask containing 7-chloro-1-{[(1R,2R,4R)-4-hydroxy-2-methylcyclohexyl]amino}-5H-pyrido[4,3-b]indole-4-carbonitrile (37 mg, 0.104 mmol), 1-methyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (65 mg, 0.31 mmol), Pd2(dba)3 (9.6 mg, 0.010 mmol), tricyclohexylphosphine (7.3 mg, 0.026 mmol), and K3PO4 (1.27 M, 0.28 mL, 0.35 mmol) was evacuated and refilled with nitrogen (×3). Dioxane (3 mL) was added to the mixture, and the resultant reaction mixture was heated to 100° C. overnight, and purified by flash chromatography to afford the title compound. LRMS (APCI) calc'd for (C23H24N6O) [M+H]+, 401.2. found 401.1.

Provenance & Evidence