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
反応式
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]1参加物
3
実験手順
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
出典と根拠
- ORDレコード
- ord-17f00d24fb2e43b2bfecf3fadb492dc6
- 出典データセット
- uspto-grants-2012_02
- 特許番号
- US08124602B2
反応ノート
読み込み中…