1,4-Diazepan-5-one → 1-[(E)-3-(4-Chloro-3-fluoro-phenyl)-acryloyl]-[1,4]diazepan-5-one
Reaction equation
[Cl:1][C:2]1[CH:12]=[CH:11][C:5](/[CH:6]=[CH:7]/[C:8]([OH:10])=O)=[CH:4][C:3]=1[F:13].[NH:14]1[CH2:20][CH2:19][C:18](=[O:21])[NH:17][CH2:16][CH2:15]1>>[Cl:1][C:2]1[CH:12]=[CH:11][C:5](/[CH:6]=[CH:7]/[C:8]([N:14]2[CH2:20][CH2:19][C:18](=[O:21])[NH:17][CH2:16][CH2:15]2)=[O:10])=[CH:4][C:3]=1[F:13]Participants
3
Procedure
In analogy to the procedure described for intermediate 1A, (E)-4-chloro-3-fluorocinnamic acid and 2,3,6,7-tetrahydro-(1H)-1,4-diazepin-5(4H)-one gave the title compound as white solid. MS: 297.3 (MH+).
Sources & evidence
- ORD record
- ord-a87af4bccd0a4ca19acc41560733e115
- Source dataset
- uspto-grants-2009_12
- Patent number
- US07632829B2
Reaction notes
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