Reaktionsgleichung
[NH2:1][CH2:2][CH2:3][NH:4][C:5]1[CH:10]=[CH:9][CH:8]=[CH:7][N:6]=1.Cl[C:12]1C=CC=[CH:14][N:13]=1.[CH2:18]([NH2:21])[CH2:19]N.N1[C:26]2[CH:27]=[CH:28][CH:29]=[C:30]([C:31]([NH2:33])=[NH2+])[C:25]=2N=N1.CCN(C(C)C)C(C)C.CC[O:45]CC>C(#N)C>[N:6]1[CH:7]=[CH:8][CH:9]=[CH:10][C:5]=1[NH:4][CH2:3][CH2:2][NH:1][C:12]1[N:21]=[C:18]([C:27]2[CH:26]=[CH:25][C:30]([C:31]([NH2:33])=[O:45])=[CH:29][CH:28]=2)[CH:19]=[CH:14][N:13]=1Komponenten
Edukt 6
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Versuchsvorschrift
2-(2-Aminoethylamino)pyridine (prepared from 2-chloropyridine and ethylenediamine in accordance with the method described in T. Mega et al., 1988, Bull. Chem. Soc. Japan 61:4315, which is incorporated herein by reference) (6 mmol) was treated with benzotriazole carboxamidinium 4-methylbenzenesulfonatesulfonate (2.0 g, 6 mmol) and DIEA (1.05 ml, 6 mmol) in anhydrous acetonitrile (10 ml) for 65 hours. Ether (ca. 10 ml) was then added to this mixture. After 8 hours the white solid amino[2-(2-pyridylamino)ethyl]carboxamidinium 4-methylbenzenesulfonate was filtered off and dried in vacuo. The resulting guanidine (200 mg) was reacted with 100 mg of resin (21 hours, 90° C.) according to the method described in Example 10 (Resin method C), to give the title compound.
Aufarbeitung
- filtrationAfter 8 hours the white solid amino[2-(2-pyridylamino)ethyl]carboxamidinium 4-methylbenzenesulfonate was filtered off
- customdried in vacuo
- customThe resulting guanidine (200 mg) was reacted with 100 mg of resin (21 hours, 90° C.)
Quellen und Nachweise
- ORD-Eintrag
- ord-c5bdf6da68cb40abbb85507f429e9fe9
- Quelldatensatz
- uspto-grants-2008_09
- Patentnummer
- US07425557B2
Verknüpfte Notizen
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