2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl → HCID 90341040, compound

Participants

Reaction Conditions

Reaction Steps

To a degassed solution of 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-2H-indazole-3-carboxamide (70 mg, 0.14 mmol), 2-chloro-11-fluoro-5,6-dihydroindolo[1,2-h][1,7]naphthyridine (46 mg, 0.17 mmol) and K3PO4.3H2O (112 mg, 0.42 mmol) in 1,4-dioxane (5 mL) was added Pd2(dba)3 (13 mg, 0.014 mmol) and X-Phos (14 mg, 0.028 mmol) under N2. The reaction mixture was heated to 100° C. and stirred for 3 hours, and then filtered through a celite pad. The filtrate was concentrated in vacuo, and the residue was purified by prep-HPLC to give the desired product (20 mg, yield: 24%). 1H-NMR (CDCl3, 400 MHz) δ 8.03 (s, 1H), 7.83 (s, 1H), 7.55˜7.60 (m, 1H), 7.52˜7.54 (m, 2H), 7.45 (s, 1H), 7.09˜7.19 (m, 5H), 6.73 (s, 1H), 6.30 (s, 1H), 6.20 (s, 1H), 4.28 (t, J=6.0 Hz, 2H), 3.32 (s, 3H), 3.25 (t, J=6.0 Hz, 2H), 2.92 (d, J=4.8 Hz, 3H), 2.76 (s, 3H). MS (M+H)+: 613.

Provenance & Evidence