Reaktionsgleichung
[CH:1]1[C:10]2[C:5](=[CH:6][CH:7]=[CH:8][CH:9]=2)[CH:4]=[C:3]([C:11]([NH:13][C:14]2[NH:18][C:17]3[CH:19]=[C:20]([O:26][CH2:27][CH3:28])[CH:21]=[C:22]([C:23]([OH:25])=O)[C:16]=3[N:15]=2)=[O:12])[N:2]=1.CN(C(ON1N=NC2C=CC=CC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.CCN(C(C)C)C(C)C.S(O)(O)(=O)=O.[NH2:67][C:68]1[NH:69][CH:70]=[CH:71][N:72]=1>CN(C=O)C.[Cl-].[Na+].O>[CH2:27]([O:26][C:20]1[CH:21]=[C:22]([C:23](=[O:25])[NH:67][C:68]2[NH:69][CH:70]=[CH:71][N:72]=2)[C:16]2[NH:15][C:14]([NH:13][C:11]([C:3]3[N:2]=[CH:1][C:10]4[C:5]([CH:4]=3)=[CH:6][CH:7]=[CH:8][CH:9]=4)=[O:12])=[N:18][C:17]=2[CH:19]=1)[CH3:28]Komponenten
7
Edukt 4
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 2
Versuchsvorschrift
100 mg (0.3 mmol) of 2-[(isoquinoline-3-carbonyl)-amino]-6-ethoxy-1H-benzoimidazole-4-carboxylic acid and 200 mg (0.53 mmol) of HBTU were dissolved in 1.0 mL of DMF and 0.5 mL of DIEA and reacted with 132 mg (1.0 mmol) of 2-aminoimidazole sulfate as described in general procedure A. Upon completion, the reaction was diluted with brine. The resulting solid was filtered, washed with water and EtOAc, and dried under vacuum to produce 30 mg (23%) of isoquinoline-3-carboxylic acid [5-ethoxy-7-(1H-imidazol-2-ylcarbamoyl)-1H-benzoimidazol-2-yl]-amide . LCMS: 443 (M+1)+.
Aufarbeitung
- filtrationThe resulting solid was filtered
- washwashed with water and EtOAc
- customdried under vacuum
Quellen und Nachweise
- ORD-Eintrag
- ord-db2fe9b4650b46a692ec60a0cb00b2a2
- Quelldatensatz
- uspto-grants-2015_02
- Patentnummer
- US08946259B2
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