(RS)-3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl]-phenyl}-propionic acid tert-butyl ester → (RS)-[2-Dimethylamino-2',3'-difluoro-5-(3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl]-phenyl}-propionylamino)-biphenyl-4-yl]-carbamic acid tert.-butyl ester
Reaction equation
[C:1]([O:5][C:6](=[O:26])[NH:7][C:8]1[C:13]([NH2:14])=[CH:12][C:11]([C:15]2[CH:20]=[CH:19][CH:18]=[C:17]([F:21])[C:16]=2[F:22])=[C:10]([N:23]([CH3:25])[CH3:24])[CH:9]=1)([CH3:4])([CH3:3])[CH3:2].C([O:31][C:32](=O)[CH2:33][C:34](=[O:54])[C:35]1[CH:40]=[CH:39][CH:38]=[C:37]([N:41]2[C:45]([CH2:46][O:47][CH:48]3[CH2:53][CH2:52][CH2:51][CH2:50][O:49]3)=[CH:44][N:43]=[N:42]2)[CH:36]=1)(C)(C)C>>[C:1]([O:5][C:6](=[O:26])[NH:7][C:8]1[C:13]([NH:14][C:32](=[O:31])[CH2:33][C:34](=[O:54])[C:35]2[CH:40]=[CH:39][CH:38]=[C:37]([N:41]3[C:45]([CH2:46][O:47][CH:48]4[CH2:53][CH2:52][CH2:51][CH2:50][O:49]4)=[CH:44][N:43]=[N:42]3)[CH:36]=2)=[CH:12][C:11]([C:15]2[CH:20]=[CH:19][CH:18]=[C:17]([F:21])[C:16]=2[F:22])=[C:10]([N:23]([CH3:24])[CH3:25])[CH:9]=1)([CH3:4])([CH3:3])[CH3:2]Participants
3
Reactant 2
Product 1
Procedure
The title compound was prepared from (5-amino-2-dimethylamino-2′,3′-difluoro-biphenyl-4-yl)-carbamic acid tert.-butyl ester (Example J3) and (RS)-3-oxo-3-{3-[5-(tetrahydro-pyran-2-yloxymethyl)-[1,2,3]triazol-1-yl ]-phenyl}-propionic acid tert-butyl ester (Example K5) according to the general procedure M. Obtained as a yellow solid (253 mg).
Sources & evidence
- ORD record
- ord-afcdd2fadc20423985a3809c7296dc07
- Source dataset
- uspto-grants-2003_04
- Patent number
- US06544985B2
Reaction notes
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