2-Dicyclohexylphosphino-2',4',6'-triisoprophylbiphenyl → HCID 71509398, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-chloro-11-fluoro-6H-benzo[5,6][1,3]oxazino[3,4-a]indole (30 mg, 0.11 mmol), 2-(4-fluorophenyl)-N-methyl-6-(N-methylmethylsulfonamido)-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)benzofuran-3-carboxamide (55 mg, 0.11 mmol), K3PO4.3H2O (88 mg, 0.33 mmol), Pd2(dba)3 (10 mg, 0.011 mmol), X-Phos (11 mg, 0.022 mmol) was stirred in dixane/H2O (5 mL, 4:1) at 110° C. for 12 hours. Then the mixture was cooled to 25° C., water was added to it. The mixture was extracted with ethyl acetate and washed with brine, dried over Na2SO4. After the combined organic layers were concentrated, the resulting residue was purified using prep-TLC (petroleum ether:EtOAc=3:1) to provide the product of Compound 43 (25 mg, yield: 40%). 1H-NMR (CDCl3, 400 MHz) δ 9.94˜7.97 (m, 2H), 7.83˜7.86 (m, 2H), 7.62 (s, 1H), 7.37˜7.40 (m, 1H), 7.09˜7.24 (m, 5H), 6.93 (s, 1H), 6.80˜6.85 (m, 1H), 5.95 (s, 2H), 5.85 (br, 1H), 3.16 (s, 3H), 3.00˜3.01 (d, J=5.2 Hz, 3H), 2.78 (s, 3H). MS (M+H)+: 614.

Provenance & Evidence