Ammonia → 2-{5-Amino-3-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-1,2,4-triazin-6-yl}-2-fluoropropanamide

Participants

Reaction Steps

250 mg (0.522 mmol) of ethyl 2-fluoro-2-{3-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]-5-hydroxy-1,2,4-triazin-6-yl}propanoate were admixed with 3 ml of phosphoryl chloride and stirred overnight at RT. The reaction mixture was diluted with 10 ml of dry acetonitrile and, with ice-cooling, stirred into 5 ml of concentrated aqueous ammonia solution (35% strength). Stirring was continued for 2 h at RT and for 16 h at 50° C. After cooling, the precipitate was filtered off with suction and dried in vacuo. This gave 294 mg (purity 95%, quant. yield) of the target compound.

Provenance & Evidence