Water → HCID 68157785, compound

Participants

Reaction Conditions

Reaction Steps

Triethylamine (518 μl, 3.72 mol) was added to (S)-2-amino-N-[4-fluoro-2-(pyrimidin-2-ylamino)phenyl]propionamide hydrochloride salt 161b (289 mg, 0.93 mmol) and 6-chloro-9-(tetrahydropyran-2-yl)purine (265 mg, 1.10 mol) in IPA (5.0 ml) and heated to 80° C. overnight. The reaction was poured into water and the aqueous layer extracted into EtOAc (×3). The combined organic fractions were washed with brine, dried (Na2SO4) and concentrated in vacuo. The product was purified by chromatography (SiO2, 0-10% 2M ammonia methanol/DCM) to yield the title compound as a 1:1 mixture of diastereomers (236 mg, 0.50 mmol, 53%). LCMS RT 2.63 min [M+H]+ 478.2.

Provenance & Evidence