1-((4-methoxyphenyl)methyl)-1H-pyrazol-4-amine → 2-[5-[1-(4-Methoxy-benzyl)-1H-pyrazol-4-ylcarbamoyl]-2-oxo-1-(2-trimethylsilanyl-ethoxymethyl)-1,2-dihydro-pyridin-3-yl]-indole-1-carboxylic acid tert-butyl ester
Reaktionsgleichung
[C:1]([O:5][C:6]([N:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH:10]=[C:9]1[C:17]1[C:18](=[O:34])[N:19]([CH2:26][O:27][CH2:28][CH2:29][Si:30]([CH3:33])([CH3:32])[CH3:31])[CH:20]=[C:21]([C:23]([OH:25])=O)[CH:22]=1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[CH3:35][O:36][C:37]1[CH:49]=[CH:48][C:40]([CH2:41][N:42]2[CH:46]=[C:45]([NH2:47])[CH:44]=[N:43]2)=[CH:39][CH:38]=1>>[C:1]([O:5][C:6]([N:8]1[C:16]2[C:11](=[CH:12][CH:13]=[CH:14][CH:15]=2)[CH:10]=[C:9]1[C:17]1[C:18](=[O:34])[N:19]([CH2:26][O:27][CH2:28][CH2:29][Si:30]([CH3:32])([CH3:33])[CH3:31])[CH:20]=[C:21]([C:23](=[O:25])[NH:47][C:45]2[CH:44]=[N:43][N:42]([CH2:41][C:40]3[CH:48]=[CH:49][C:37]([O:36][CH3:35])=[CH:38][CH:39]=3)[CH:46]=2)[CH:22]=1)=[O:7])([CH3:2])([CH3:3])[CH3:4]Komponenten
3
Edukt 2
Produkt 1
Versuchsvorschrift
The title compound was prepared according to the experimental used in Example 1, Step 4 using intermediate (1c) and 1-(4-methoxy-benzyl)-1H-pyrazol-4-ylamine. After the usual aqueous work up, the resultant crude product was purified by flash chromatography on SiO2 eluting with hexane—50% ethyl acetate/hexane. This afforded the title compound as a pink solid, 180 mg, 50%.