HCID 57919133, compound → HCID 68992089, compound

Participants

Reaction Steps

Using the method described in Example 49, 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-3-(tetrahydro-pyran-4-yl)-propionic acid (Intermediate 32) and 1-((R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-ylamine (Intermediate 4) afforded 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-N-[1-((R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-yl]-3-(tetrahydro-pyran-4-yl)-propionamide as an off-white solid as a mixture of diastereomers (0.60 g, 53%); ES+-HRMS m/e calcd for C27H31N5O6F2 [M+H+] 560.2315 found 560.2319. 1H NMR (400 MHz, DMSO-d6) δ ppm 1.13-1.29 (m, 2H), 1.25 (s, 3H), 1.30, 1.31 (2×s, 3H), 1.35-1.59 (m, 3H), 1.84-1.94 (m, 1H), 2.15-2.26 (m, 1H), 3.09-3.27 (m, 2H), 3.70-3.85 (m, 3H), 3.97-4.18 (m, 3H), 4.31-4.40 (m, 1H), 5.54 (dd, J=11.1, 4.0 Hz, 1H), 6.04 (d, J=2.7 Hz, 1H), 6.39 (d, J=2.1 Hz, 1H), 7.34-7.43 (m, 2H), 7.43-7.53 (m, 1H), 7.60 (br s, 1H), 8.29 (d, J=2.7 Hz, 1H), 10.86, 10.87 (2×s, 1H).

Provenance & Evidence