Dimethylamine → 4-[(Dimethylamino)methyl]-6-methoxy-1-(phenylsulfonyl)-1H-indol-5-ol

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Reaction Conditions

Reaction Steps

Paraformaldehyde (28 mg, 0.932 mmol) and 2 M Me2NH in MeOH (0.47 ml, 0.932 mmol) was heated until clear solution was obtained. The solution was added to 6-methoxy-1-(phenylsulfonyl)-1H-indol-5-ol (61 mg, 0.201 mmol; Intermediate 101) in EtOH (1.5 ml) and the mixture was heated in microwave oven at 80° C. for 10 min. A small part was purified on Gilson HPLC using 25-55% MeCN in 50 nM ammonium hydrogencarbonate as eluent. Yield: 3.8 mg; white solid. MS (ESI+) for C18H20N2O4S m/z 361 (M+H)+.

Provenance & Evidence