HCID 57919097, compound → HCID 66892811, compound

Participants

Reaction Steps

Using the method described in Example 49, 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-4-methyl-pentanoic acid (Intermediate 28) 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]-4-methyl-pentanoic acid [1-((R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-yl]-amide as an off-white solid as a mixture of diastereoisomers (1.21 g, 79%); ES+-HRMS m/e calcd for C25H29N5O5F2 [M+H+] 518.2210 found 518.2214. 1H NMR (400 MHz, DMSO-d6) δ ppm 0.87 (d, J=6.6 Hz, 3H), 0.89 (d, J=6.6 Hz, 3H), 1.25 (s, 3H), 1.30, 1.31 (2×s, 3H), 1.38-1.51 (m, 1H), 1.74-1.85 (m, 1H), 2.12-2.24 (m, 1H), 3.74 (dd, J=8.4, 5.9 Hz, 1H), 3.97-4.17 (m, 3H), 4.35 (m, 1H), 5.52 (dd, J=11.2, 4.2 Hz, 1H), 6.04 (d, J=2.7 Hz, 1H), 6.39 (d, J=2.1 Hz, 1H), 7.35-7.43 (m, 2H), 7.43-7.55 (m, 1H), 7.60 (m, 1H), 8.28 (d, J=2.7 Hz, 1H), 10.85 (s, 1H).

Provenance & Evidence