1-[6-(2,2,2-Trifluoroethoxy)-pyridin-3-yl]-ethylamine hydrochloride → 2-amino-6-methoxy-N-(1-(6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethyl)isonicotinamide
Reaction equation
Cl.[F:2][C:3]([F:16])([F:15])[CH2:4][O:5][C:6]1[N:11]=[CH:10][C:9]([CH:12]([NH2:14])[CH3:13])=[CH:8][CH:7]=1.[NH2:17][C:18]1[CH:19]=[C:20]([CH:24]=[C:25]([O:27][CH3:28])[N:26]=1)[C:21](O)=[O:22]>>[NH2:17][C:18]1[CH:19]=[C:20]([CH:24]=[C:25]([O:27][CH3:28])[N:26]=1)[C:21]([NH:14][CH:12]([C:9]1[CH:10]=[N:11][C:6]([O:5][CH2:4][C:3]([F:2])([F:15])[F:16])=[CH:7][CH:8]=1)[CH3:13])=[O:22]Participants
3
Procedure
The title compound is prepared in 65% yield (187 mg, a white solid) from (−)-1-(6-(2,2,2-trifluoroethoxy)pyridin-3-yl)ethanamine hydrochloride (200 mg, 0.78 mmol, Amine-1, single enantiomer) and 2-amino-6-methoxyisonicotinic acid (131 mg, 0.78 mmol) by the similar manner in Step-1 of Example-8.
Sources & evidence
- ORD record
- ord-59877cf4dba7476085ce58646341d29a
- Source dataset
- uspto-grants-2016_04
- Patent number
- US09302991B2
Reaction notes
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