Water → 1-Methyl-6-tosyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridine

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Reaction Steps

A mixture of 60 wt % NaH (1.74 g, 43.6 mmol) in DMF (70 mL) at 0° C. was treated with a mixture of 1-methyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridine (5.00 g, 29.0 mmol) in DMF (20 mL). After 20 min, TsCl (8.30 g, 43.6 mmol) was added. After 2 h, water (90 mL) was added and the precipitate formed was collected by filtration to give 1-methyl-6-tosyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridine (9.0 g, 95%): LC/MS (Table 2, Method c) Rt=1.44 min; MS m/z 327 (M+H)+

Provenance & Evidence