N-(2-Morpholino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-YL)phenyl)methanesulfonamide → N-(5-(3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-morpholinophenyl) methanesulfonamide

Participants

Reaction Steps

Using similar reaction conditions as described in step-ii of example-1, 5-bromo-3-(1-(3-fluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine Compound of step-I in Example 9) (200 mg, 0.3809 mmol) was coupled with N-(2-morpholino-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)methane sulfonamide (Intermediate 20) (220 mg, 0.5714 mmol), Pd(PPh3)2Cl2 (13.5 mg, 0.01904 mmol), Toluene/ethanol/water (20/10/4 ml) to afford 240 mg (90.2% yield) of the titled compound.

Provenance & Evidence