Sodium Carbonate → N-(5-(3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)-2-methoxyphenyl)methane sulfonamide

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Reaction Steps

Using similar reaction conditions as described in step-ii of example-1, 5-bromo-3-(1-(3,5-difluorobenzyl)-1H-pyrazol-4-yl)-1-tosyl-1H-pyrrolo[2,3-b]pyridine (200 mg, 0.3683 mmol) was coupled with N-(2-methoxy-5-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl methane sulfonamide (Intermediate 17), (120 mg, 0.368 mmol) using sodium carbonate (117 mg, 1.1049 mmol) and Pd(PPh3)2Cl2 (14 mg, 0.0184 mmol) in DME/water (15/2 ml). This afforded 107 mg (43.8% yield) after purification by column (Silica gel 230/400) using 65% ethyl acetate in hexane as eluent. MS: m/z=664.1 (M+1).

Provenance & Evidence