Benzotriazol-1-yl 2-amino-6-fluoro-pyrazolo[1,5-a]pyrimidine-3-carboxylate → (R)-2-amino-6-fluoro-N-(4-((1-methylpiperidin-3-yl)oxy)pyrimidin-5-yl)pyrazolo[1,5-a]pyrimidine-3-carboxamide

Participants

Reaction Steps

A solution of benzotriazol-1-yl 2-amino-6-fluoro-pyrazolo[1,5-a]pyrimidine-3-carboxylate 6a (125 mg, 0.3990 mmol) and 4-[[(3R)-1-methyl-3-piperidyl]oxy]pyrimidin-5-amine 7a (83.10 mg, 0.3990 mmol) in NMP (2 mL) was heated at 100° C. overnight. The reaction mixture was cooled to RT, passed through a SCX cartridge, eluting with 2M ammonia in methanol. The product fractions were combined, concentrated in vacuo and purified by HPLC. The title product I-A-1 was isolated (60 mg., 38.9%)

Provenance & Evidence