3-cyclopentyl-2-(4-cyclopentylmethoxy-6-oxo-6H-pyridazin-1-yl)-propionic acid → 3-cyclopentyl-2-(4-cyclopentylmethoxy-6-oxo-6H-pyridazin-1-yl)-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-propionamide

Participants

Reaction Steps

Using the method described in Example 1, 3-cyclopentyl-2-(4-cyclopentylmethoxy-6-oxo-6H-pyridazin-1-yl)-propionic acid (Intermediate 59) and 1-(3-amino-pyrazol-1-yl)-2-methyl-propan-2-ol (Intermediate 1) afforded 3-cyclopentyl-2-(4-cyclopentylmethoxy-6-oxo-6H-pyridazin-1-yl)-N-[1-(2-hydroxy-2-methyl-propyl)-1H-pyrazol-3-yl]-propionamide as a white solid (22.2 mg, 10%); ES+-HRMS m/e calcd for C25H37N5O4 [M+H+] 472.2919, found 472.2922. 1H-NMR (400 MHz, DMSO-d6) δ ppm 1.05 (s, 3H), 1.06 (s, 3H), 1.05 (m, 1H), 1.25-1.97 (m, 18H), 2.26 (m, 1H), 3.89 (s, 2H), 3.90 (d, J=5.8 Hz, 2H), 4.67 (s, 1H), 5.46 (dd, J=4.2, J=11.2 Hz, 1H), 6.27 (d, J=2.8 Hz, 1H), 6.39 (d, J=2.2 Hz, 1H), 7.52 (d, J=2.2 Hz, 1H), 7.82 (d, J=2.8 Hz, 1H), 10.73 (s, 1H).

Provenance & Evidence