反应详情

Using similar reaction conditions as described in step-ii of example-1, tert-butyl 4-(3-(3-iodo-1-tosyl-1H-pyrrolo[2,3-b]pyridin-5-yl)phenyl)piperazine-1-carboxylate (intermediate 39) (250 mg, 0.379 mmol) was coupled with 1-(3-fluorobenzyl)-3,5-dimethyl-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazole (intermediate 16) (220 mg, 0.666 mmol) in sodium carbonate (121 mg, 1.139 mmol), Pd(PPh3)2Cl2 (13.3 mg, 0.0189 mmol), toluene/ethanol/water (25/12.5/6 ml). This afforded 267 g (60% yield) after purification by column (Silica gel 60/120) using 1.5% of methanol in chloroform as eluent. MS: m/z=735.3 (M+1).

1. customreaction conditions
2. customThis afforded 267 g (60% yield) after purification by column (Silica gel 60/120)