1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → 1-(2-bromo-5H-pyrrolo[3,2-b]pyrazin-7-yl)-2-(1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-ylamino)ethanone

Participants

Reaction Conditions

Reaction Steps

A mixture of 2-bromo-5H-pyrrolo[3,2-b]pyrazine-7-carboxylic acid (2.5 g, 10.33 mmol), 1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-amine (2.52 g, 12.4 mmol), EDCI (1.97 g, 10.33 mmol), HOBt (2.8 g, 20.6 mmol) and DIPEA (2.7 g, 20.66 mmol) in dry DMF (30 mL) was heated to 30° C. for 16 hours. Then water (30 mL) was added, the formed precipitate was separated by filtration and the filter cake was washed with water (10 mL) and dried to afford 1-(2-bromo-5H-pyrrolo[3,2-b]pyrazin-7-yl)-2-(1-(tert-butyldimethylsilyloxy)-2-methylpropan-2-ylamino)ethanone (2.7 g, 61%) as a yellow solid. LCMS: (M+H)+=427.

Provenance & Evidence