2-Aminothiazole → 3-[2-(4-Fluoro-phenyl)-pyrimidin-5-yl]-N-(thiazol-2-yl)-acrylamide
Reaction equation
[F:1][C:2]1[CH:7]=[CH:6][C:5]([C:8]2[N:13]=[CH:12][C:11]([CH:14]=[CH:15][C:16]([OH:18])=O)=[CH:10][N:9]=2)=[CH:4][CH:3]=1.[NH2:19][C:20]1[S:21][CH:22]=[CH:23][N:24]=1.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.C(N(CC)CC)C>>[F:1][C:2]1[CH:3]=[CH:4][C:5]([C:8]2[N:9]=[CH:10][C:11]([CH:14]=[CH:15][C:16]([NH:19][C:20]3[S:21][CH:22]=[CH:23][N:24]=3)=[O:18])=[CH:12][N:13]=2)=[CH:6][CH:7]=1Participants
5
Reactant 4
Product 1
Procedure
The compound was prepared as described in Example 116(d) from 39 mg (0.16 mmol) of 3-[2-(4-fluoro-phenyl)-pyrimidin-5-yl]-acrylic acid, 32 mg (0.32 mmol) of 2-aminothiazole, 267 mg (0.68 mmol) of HATU and 65 mg (0.64 mmol) of triethylamine. Yield: 4 mg.
Workup
- customThe compound was prepared
Sources & evidence
- ORD record
- ord-e6bbab5886904fb9ae26e5831e10e425
- Source dataset
- uspto-grants-2012_11
- Patent number
- US08304438B2
Reaction notes
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