Reaktionsgleichung
C(=O)([O-])[O-].[K+].[K+].[F-].[Cs+].[CH:9]1([NH:12][C:13](=[O:39])[C:14]2[CH:19]=[CH:18][C:17]([CH3:20])=[C:16]([N:21]3[CH:26]=[CH:25][N:24]=[C:23]([NH:27][C:28]4([C:31]5[CH:36]=[CH:35][CH:34]=[CH:33][C:32]=5[OH:37])[CH2:30][CH2:29]4)[C:22]3=[O:38])[CH:15]=2)[CH2:11][CH2:10]1.[N+](C1C=C(S(O[CH2:53][C@H:54]2[CH2:56][O:55]2)(=O)=O)C=CC=1)([O-])=O>CN(C=O)C>[CH:9]1([NH:12][C:13](=[O:39])[C:14]2[CH:19]=[CH:18][C:17]([CH3:20])=[C:16]([N:21]3[CH:26]=[CH:25][N:24]=[C:23]([NH:27][C:28]4([C:31]5[CH:36]=[CH:35][CH:34]=[CH:33][C:32]=5[O:37][CH2:53][C@H:54]5[CH2:56][O:55]5)[CH2:30][CH2:29]4)[C:22]3=[O:38])[CH:15]=2)[CH2:11][CH2:10]1Komponenten
6
Versuchsvorschrift
Potassium carbonate (216 mg) and cesium fluoride (36.5 mg) were added to N-cyclopropyl-3-(3-(1-(2-hydroxyphenyl)cyclopropylamino)-2-oxopyrazin-1(2H)-yl)-4-methylbenzamide (Example 167d, 500 mg) in DMF (9 mL) and stirred for 1 h. (R)-oxiran-2-ylmethyl 3-nitrobenzenesulfonate (311 mg) was added and the reaction stirred for 3 days. The reaction mixture was used without isolation/purification.
Aufarbeitung
- additionwas added
- customThe reaction mixture was used without isolation/purification
Quellen und Nachweise
- ORD-Eintrag
- ord-bea578bc2d2d4900aded24217eb37849
- Quelldatensatz
- uspto-grants-2014_11
- Patentnummer
- US08889692B2
Verknüpfte Notizen
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