Trifluoroacetic acid → HCID 89601244, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of 4-(5-(5-chloro-1-(4-methoxybenzyl)-2-oxo-1,2-dihydropyridin-3-yl)-2-(2-(dimethylamino)-4-methoxypyrimidin-5-yl)-3-isopropyl-6-oxo-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-4-yl)-2-fluorobenzonitrile (388 mg, 0.568 mmol, product from step 193.1) and TFA (2.188 ml, 28.4 mmol) was stirred at 100° C. for 1 hour. Then the reaction mixture was quenched with a saturated NaHCO3 solution and extracted twice with CH2Cl2. The organic layers were combined and washed with saturated NaHCO3 solution, dried (Na2SO4) and evaporated. The reaction mixture was purified by chromatography (Silicagel, EtOAc). After evaporation of the fractions, the residue was triturated in diisopropylether to afford 121 mg (0.215 mmol, 37.8% yield) of the title compound as a white solid. LCMS: (M+H)=563/565; tR=1.04 min (LC−MS 4). TLC: Rf=0.34 (EtOAc). 1H−NMR (DMSO−d6, 600 MHz) δ ppm 12.36 (s, 1H) 8.28 (s, 1H) 7.91 (t, 1H) 7.65−7.53 (m, 3H) 7.40 (d, 1H) 6.84 (bs, 1H) 3.87 (s, 3H) 3.18 (s, 6H) 2.60 (m, 1H) 1.08 (d, 3H) 0.47 (d, 3H).

Provenance & Evidence