1-(3-amino-1H-pyrazol-1-yl)-2-methylpropan-2-ol → 3-cyclopentyl-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-2-(1-oxo-1H-phthalazin-2-yl)-propionamide

Participants

Reaction Steps

Using the method described in Example 83, Step 3,3-cyclopentyl-2-(1-oxo-1H-phthalazin-2-yl)-propionic acid (as prepared in Example 83, Step 2) and 1-(3-amino-pyrazol-1-yl)-2-methyl-propan-2-ol (Intermediate 1) afforded 3-cyclopentyl-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-2-(1-oxo-1H-phthalazin-2-yl)-propionamide as a white solid (48 mg, 11%); ES+-HRMS m/e calcd for C23H29N5O3 [M+H+] 319.1223 found 319.1223. 1H-NMR (300 MHz, DMSO-d6) δ ppm 1.03 (s, 6H), 1.04-1.17 (m, 1H), 1.24-1.72 (m, 8H), 1.93-2.10 (m, 1H), 2.21-2.35 (m, 1H), 3.86 (s, 2H), 4.64 (s, 1H), 5.61 (dd, J=10.7, 4.1 Hz, 1H), 6.39 (d, J=2.1 Hz, 1H), 7.50 (d, J=2.1 Hz, 1H), 7.79-7.91 (m, 1H), 7.91-7.98 (m, 2H), 8.24 (d, J=7.5 Hz, 1H), 8.48 (s, 1H), 10.66 (s, 1H).

Provenance & Evidence