HCID 57919339, compound → HCID 68991072, compound
Reaction equation
[F:1][C:2]1[CH:28]=[CH:27][CH:26]=[C:25]([F:29])[C:3]=1[O:4][C:5]1[CH:6]=[N:7][N:8]([CH:12]([CH2:16][C:17]2[C:22]([F:23])=[CH:21][CH:20]=[CH:19][C:18]=2[F:24])[C:13](O)=[O:14])[C:9](=[O:11])[CH:10]=1.[CH3:30][C:31]1([CH3:43])[O:35][C@H:34]([CH2:36][N:37]2[CH:41]=[CH:40][C:39]([NH2:42])=[N:38]2)[CH2:33][O:32]1>>[F:29][C:25]1[CH:26]=[CH:27][CH:28]=[C:2]([F:1])[C:3]=1[O:4][C:5]1[CH:6]=[N:7][N:8]([CH:12]([CH2:16][C:17]2[C:18]([F:24])=[CH:19][CH:20]=[CH:21][C:22]=2[F:23])[C:13]([NH:42][C:39]2[CH:40]=[CH:41][N:37]([CH2:36][C@@H:34]3[CH2:33][O:32][C:31]([CH3:43])([CH3:30])[O:35]3)[N:38]=2)=[O:14])[C:9](=[O:11])[CH:10]=1Participants
3
Procedure
Using the method described in Example 49, 2-[4-(2,6-difluoro-phenoxy)-6-oxo-6H-pyridazin-1-yl]-3-(2,6-difluoro-phenyl)-propionic acid (Intermediate 34) 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]-3-(2,6-difluoro-phenyl)-N-[1-((R)-2,2-dimethyl-[1,3]dioxolan-4-ylmethyl)-1H-pyrazol-3-yl]-propionamide as an off-white solid as a mixture of diastereomers (367.9 mg, 59%).
Sources & evidence
- ORD record
- ord-dab78e4560f24b59a712b5436db64e80
- Source dataset
- uspto-grants-2012_09
- Patent number
- US08258134B2
Reaction notes
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