5-Cyanopyridine-2-carboxylic acid → 5-cyano-pyridine-2-carboxylic acid [4-fluoro-3-((R)-3-methyl-5-oxo-[1,4]oxazepan-3-yl)-phenyl]-amide
Reaction equation
[C:1]([C:3]1[CH:4]=[CH:5][C:6]([C:9]([OH:11])=O)=[N:7][CH:8]=1)#[N:2].Cl.[NH2:13][C:14]1[CH:15]=[CH:16][C:17]([F:29])=[C:18]([C@@:20]2([CH3:28])[NH:26][C:25](=[O:27])[CH2:24][CH2:23][O:22][CH2:21]2)[CH:19]=1>>[F:29][C:17]1[CH:16]=[CH:15][C:14]([NH:13][C:9]([C:6]2[CH:5]=[CH:4][C:3]([C:1]#[N:2])=[CH:8][N:7]=2)=[O:11])=[CH:19][C:18]=1[C@@:20]1([CH3:28])[NH:26][C:25](=[O:27])[CH2:24][CH2:23][O:22][CH2:21]1Participants
3
Procedure
Starting from 5-cyano-pyridine-2-carboxylic acid and (R)-3-(5-amino-2-fluoro-phenyl)-3-methyl-[1,4]oxazepan-5-one hydrochloride, the 5-cyano-pyridine-2-carboxylic acid [4-fluoro-3-((R)-3-methyl-5-oxo-[1,4]oxazepan-3-yl)-phenyl]-amide was obtained as a white solid. MS (ISP): m/z=369.1 [M+H]+.
Sources & evidence
- ORD record
- ord-db1148357b264a8b84c88e8291ef0c6a
- Source dataset
- uspto-grants-2014_03
- Patent number
- US08673894B2
Reaction notes
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