4-Aminotetrahydropyran → HCID 57329857, compound
Reaction equation
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:12]=[N:11][N:10]([CH3:13])[C:9]=2/[CH:14]=[CH:15]/[C:16]2[S:17][C:18]([C:22](O)=[O:23])=[C:19]([CH3:21])[N:20]=2)=[CH:4][CH:3]=1.[NH2:25][CH:26]1[CH2:31][CH2:30][O:29][CH2:28][CH2:27]1>>[O:29]1[CH2:30][CH2:31][CH:26]([NH:25][C:22]([C:18]2[S:17][C:16](/[CH:15]=[CH:14]/[C:9]3[N:10]([CH3:13])[N:11]=[N:12][C:8]=3[C:5]3[CH:4]=[CH:3][C:2]([F:1])=[CH:7][CH:6]=3)=[N:20][C:19]=2[CH3:21])=[O:23])[CH2:27][CH2:28]1Participants
3
Procedure
As described for example 6f, 2-{(E)-2-[5-(4-fluoro-phenyl)-3-methyl-3H-[1,2,3]triazol-4-yl]-vinyl}-4-methyl-thiazole-5-carboxylic acid (75 mg, 0.22 mmol), was converted, using 4-aminotetrahydropyran instead of isopropylamine, to the title compound (63 mg, 68%) which was obtained as a light yellow solid. MS: m/e=428.3 [M+H]+.
Sources & evidence
- ORD record
- ord-6ec02f560fdc44b58ed5aede6c459f43
- Source dataset
- uspto-grants-2014_04
- Patent number
- US08697696B2
Reaction notes
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