5-[(3-amino-1-methyl-1H-indazol-6-yl)oxy]-3-(4-methoxybenzyl)-3,4-dihydropyrido[2,3-d]pyrimidin-2(1H)-one → 5-(3-Amino-1-methyl-1H-indazol-6-yloxy)-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-2-one

Participants

Reaction Conditions

Reaction Steps

Compound 276 (25.00 mg; 0.06 mmol; 1.00 eq.) was dissolved in trifluoroacetic acid (2.00 ml). The vessel was sealed and heated at 75 degrees C. for two days. The reaction was concentrated, redissolved in DMSO, treated with Et3N to get pH ˜8, and then purified via prep HPLC to afford 17mg (69%) of 277 as a white solid. LC-MS (M+H=311, obsd.=311).

Provenance & Evidence