1-[2-(4-Aminopiperidin-1-yl)ethyl]-7-methoxy-1,4-dihydro-2H-3,1-benzoxazin-2-one trifluoro acetate → 1-[(2E)-3-(2,5-Difluorophenyl)prop-2-en-1-yl]piperidin-4-amine
Reaktionsgleichung
C(OC(=O)[NH:7][CH:8]1[CH2:13][CH2:12][N:11]([CH2:14]/[CH:15]=[CH:16]/[C:17]2[CH:22]=[C:21]([F:23])[CH:20]=[CH:19][C:18]=2[F:24])[CH2:10][CH2:9]1)(C)(C)C.FC(F)(F)C(O)=O.NC1CCN(CCN2C3C=C(OC)C=CC=3COC2=O)CC1>>[F:24][C:18]1[CH:19]=[CH:20][C:21]([F:23])=[CH:22][C:17]=1/[CH:16]=[CH:15]/[CH2:14][N:11]1[CH2:12][CH2:13][CH:8]([NH2:7])[CH2:9][CH2:10]1Komponenten
3
Versuchsvorschrift
tert-Butyl{1-[(2E)-3-(2,5-difluorophenyl)prop-2-en-1-yl]piperidin-4-yl}carbamate (Intermediate 123, 299 mg, 0.85 mmol) was reacted as described for Intermediate 106. The crude trifluoro acetate of the title compound was obtained as an oil, 430 mg (quantitative), and used without further purification for the next step
Quellen und Nachweise
- ORD-Eintrag
- ord-17f00d24fb2e43b2bfecf3fadb492dc6
- Quelldatensatz
- uspto-grants-2012_02
- Patentnummer
- US08124602B2
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