4-Chloro-1H-pyrazole-3-carboxylic acid → HCID 71059646, compound
Reaction equation
[F:1][C:2]1([F:19])[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][CH2:10][CH2:9]2.Cl[C:21]1[CH:22]=N[NH:24][C:25]=1[C:26]([OH:28])=O>>[NH2:8][C:5]1[O:6][CH2:7][C:2]([F:1])([F:19])[C@@:3]2([C:17]3[C:12](=[CH:13][CH:14]=[C:15]([NH:18][C:26](=[O:28])[C:25]4[CH:21]=[CH:22][C:2]([C:3]#[N:4])=[CH:7][N:24]=4)[CH:16]=3)[O:11][CH2:10][CH2:9]2)[N:4]=1Participants
3
Procedure
The condensation of (R)-5′,5′-difluoro-5′,6′-dihydrospiro[chroman-4,4′-[1,3]oxazine]-2′,6-diamine (intermediate B7.1) and 4-chloro-1H-pyrazole-5-carboxylic acid yielded the title compound (34% yield) as a pale yellow solid. MS (ISP): m/z=398.1 [M+H]+.
Sources & evidence
- ORD record
- ord-558162fdec50441c9f81f5b5b2cc9317
- Source dataset
- uspto-grants-2015_07
- Patent number
- US09079919B2
Reaction notes
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