Iodine → N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-N'-{[6-fluoro-3'-(iodomethyl)-3-biphenylyl]methyl}-1,3-benzenedicarboxamide

Participants

Reaction Steps

To a solution of N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridine-5-yl]methyl}-N′-{[6-fluoro-3′-(hydroxymethyl)-3-biphenylyl]methyl}-1,3-benzenedicarboxamide (0.0997 g, 0.15 mmol) in DCM (1.0 mL) was added iodine (0.0381 g, 0.15 mmol), and PS-PPh3 (0.0818 g, 0.18 mmol). This mixture was stirred at room temperature for 28 h, filtered and concentrated to afford N-{[1,6-diethyl-4-(tetrahydro-2H-pyran-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-5-yl]methyl}-N′-{[6-fluoro-3′-(iodomethyl)-3-biphenylyl]methyl}-1,3-benzenedicarboxamide which was carried on to the next step of the reaction directly.

Provenance & Evidence