Dimethylamine → 1-(dimethylamino)-3-(5-methoxy-3-(1-methyl-6-tosyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridin-7-yl)-1H-indol-1-yl)propan-2-ol

Participants

Reaction Steps

In a flask, a mixture of 7-(5-methoxy-1-(oxiran-2-ylmethyl)-1H-indol-3-yl)-1-methyl-6-tosyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridine (0.212 mmol) in DMF (5 mL) and dimethylamine (0.054 mL, 1.061 mmol) was stirred for about 17 h at rt. Additional dimethylamine (0.054 mL, 1.061 mmol) was added and the mixture was heated to about 50° C. for about 5 h, then at rt for about 17 h. The mixture was concentrated in vacuo to provide 1-(dimethylamino)-3-(5-methoxy-3-(1-methyl-6-tosyl-1,6-dihydropyrazolo[3,4-d]pyrrolo[2,3-b]pyridin-7-yl)-1H-indol-1-yl)propan-2-ol (0.120 g, 99%): LC/MS (Table 2, Method c) Rt=1.29 min; MS m/z 573 (M+H)+.

Provenance & Evidence