Hydrochloric Acid → HCID 46869362, compound

Participants

Reaction Steps

To a 25 ml flask was added ethyl 2-((S)-3-(4-fluorophenyl)-1-(1-methyl-3-(pyridin-4-yl)-1H-pyrazol-5-ylamino)-1-oxopropan-2-ylamino)acetate 103.1.C (331 mg, 0.78 mmole), lithium hydroxide monohydrate (65.3 mg, 1.56 mmole), 1 ml of water and 6 ml of tetrahydrofuran. After 3 hours, 0.78 ml of 2N-hydrogen chloride solution was added to neutralize. The solvent was removed by rotary evaporation. The crude product was purified by silica gel chromatography to give 103.2 (268 mg, 87% yield) as colorless amorphous. LCMS ESI (pos.) m/e: 398 (M+H); 1H NMR (400 MHz, DMSO-d6) δ ppm 8.57 (d, J=5.5 Hz, 2H), 7.72 (d, J=6.3 Hz, 2H), 7.33 (dd, J=8.4, 5.7 Hz, 2H), 7.13 (t, J=8.8 Hz, 2H), 6.81 (s, 1H), 3.66 (s, 3H), 3.58 (t, J=6.8 Hz, 1H), 3.21 (d, J=16.9 Hz, 1H), 3.11 (d, J=17.2 Hz, 1H), 3.02 (dd, J=13.6, 5.9 Hz, 1H), 2.89 (dd, J=13.6, 7.9 Hz, 1H).

Provenance & Evidence