5-Chloro-2-picolinic acid → HCID 71059490, compound
Reaction equation
[F:1][C:2]1([F:21])[CH2:7][O:6][C:5]([NH2:8])=[N:4][C@@:3]21[C:17]1[C:12](=[CH:13][CH:14]=[C:15]([NH2:18])[CH:16]=1)[O:11][C:10]([CH3:20])([CH3:19])[CH2:9]2.[Cl:22][C:23]1[CH:24]=[CH:25][C:26]([C:29](O)=[O:30])=[N:27][CH:28]=1>>[NH2:8][C:5]1[O:6][CH2:7][C:2]([F:1])([F:21])[C@@:3]2([C:17]3[C:12](=[CH:13][CH:14]=[C:15]([NH:18][C:29](=[O:30])[C:26]4[CH:25]=[CH:24][C:23]([Cl:22])=[CH:28][N:27]=4)[CH:16]=3)[O:11][C:10]([CH3:19])([CH3:20])[CH2:9]2)[N:4]=1Participants
3
Procedure
The condensation of (R)-5′,5′-difluoro-2,2-dimethyl-5′,6′-dihydrospiro[chroman-4,4′-[1,3]oxazine]-2′,6-diamine (intermediate B7.3) and 5-chloropicolinic acid yielded the title compound (85% yield) as a white solid. MS (ISP): m/z=437.1 [M+H]+.
Sources & evidence
- ORD record
- ord-788a74f688f349dcae9248800cf6f870
- Source dataset
- uspto-grants-2015_07
- Patent number
- US09079919B2
Reaction notes
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