Reaktionsgleichung
[CH3:1][O:2][C:3]1[CH:4]=[CH:5][C:6]2[NH:12][C:11](=[O:13])[N:10]([CH:14]3[CH2:19][CH2:18][N:17]([C:20]4[N:25]=[CH:24][N:23]=[C:22]([C:26]([O:28]C(C)(C)C)=[O:27])[C:21]=4[CH3:33])[CH2:16][CH2:15]3)[CH2:9][CH2:8][C:7]=2[CH:34]=1.FC1C=C2C(=CC=1)NCC2.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.[B-](F)(F)(F)F>CN(C=O)C>[CH3:1][O:2][C:3]1[CH:4]=[CH:5][C:6]2[NH:12][C:11](=[O:13])[N:10]([CH:14]3[CH2:15][CH2:16][N:17]([C:20]4[N:25]=[CH:24][N:23]=[C:22]([C:26]([OH:28])=[O:27])[C:21]=4[CH3:33])[CH2:18][CH2:19]3)[CH2:9][CH2:8][C:7]=2[CH:34]=1Komponenten
5
Edukt 3
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Versuchsvorschrift
70 mg (0.17 mmol) tert. butyl 6-[4-(7-methoxy-2-oxo-1,2,4,5-tetrahydro-1,3-benzodiazepin-3-yl)-piperidin-1-yl]-5-methyl-pyrimidin-4-carboxylate, 26 mg (0.19 mmol) 5-fluoroindoline, 61 mg (0.19 mmol) TBTU and 27 μL (0.19 mmol) TEA were stirred in 1.0 mL DMF for 3 h at RT. The reaction mixture was purified by HPLC. The product-containing fractions were combined and freeze-dried.
Aufarbeitung
- customThe reaction mixture was purified by HPLC
- customfreeze-dried
Quellen und Nachweise
- ORD-Eintrag
- ord-a503c57dd4264e0c8f32ab98bd540b0c
- Quelldatensatz
- uspto-grants-2014_09
- Patentnummer
- US08829006B2
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