Diisopropylethylamine → 4-amino-N-[(3R)-1-ethylpyrrolidin-3-yl]-3-methoxy-benzamide
Reaktionsgleichung
[NH2:1][C:2]1[CH:10]=[CH:9][C:5]([C:6]([OH:8])=O)=[CH:4][C:3]=1[O:11][CH3:12].[CH2:13]([N:15]1[CH2:19][CH2:18][C@@H:17]([NH2:20])[CH2:16]1)[CH3:14].CCN(C(C)C)C(C)C.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>CN(C=O)C>[NH2:1][C:2]1[CH:10]=[CH:9][C:5]([C:6]([NH:20][C@@H:17]2[CH2:18][CH2:19][N:15]([CH2:13][CH3:14])[CH2:16]2)=[O:8])=[CH:4][C:3]=1[O:11][CH3:12]Komponenten
6
Edukt 4
Produkt 1
Reagenzien, Katalysatoren, Lösungsmittel 1
Versuchsvorschrift
To a solution of 4-amino-3-methoxybenzoic acid (Aldrich; 424 mg, 2.54 mmol) and (3R)-1-ethylpyrrolidin-3-amine (Intermediate 246; 312 mg, 2.73 mmol) in DMF (10 mL) was added DIPEA (1.4 ml, 8.04 mmol). The resultant solution was treated with HATU (1.21 g, 3.18 mmol) and stirred, under nitrogen, at ambient temperature overnight.
Quellen und Nachweise
- ORD-Eintrag
- ord-637585bed9cf47c88c084a6732adfd7e
- Quelldatensatz
- uspto-grants-2010_05
- Patentnummer
- US07709471B2
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