Cesium carbonate → Methyl cis(+/-)-3-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-4-fluorobenzoate

HRID 43794

반응식

HRID 43794 반응식
[CH3:1][O:2][C@H:3]1[C@@H:8]([NH:9][C:10](=[O:19])[O:11][CH2:12][C:13]2[CH:18]=[CH:17][CH:16]=[CH:15][CH:14]=2)[CH2:7][CH2:6][NH:5][CH2:4]1.Br[C:21]1[CH:22]=[C:23]([CH:28]=[CH:29][C:30]=1[F:31])[C:24]([O:26][CH3:27])=[O:25].C1C=CC(P(C2C(C3C(P(C4C=CC=CC=4)C4C=CC=CC=4)=CC=C4C=3C=CC=C4)=C3C(C=CC=C3)=CC=2)C2C=CC=CC=2)=CC=1.C(=O)([O-])[O-].[Cs+].[Cs+]>C([O-])(=O)C.[Pd+2].C([O-])(=O)C>[CH2:12]([O:11][C:10]([NH:9][C@H:8]1[CH2:7][CH2:6][N:5]([C:21]2[CH:22]=[C:23]([CH:28]=[CH:29][C:30]=2[F:31])[C:24]([O:26][CH3:27])=[O:25])[CH2:4][C@H:3]1[O:2][CH3:1])=[O:19])[C:13]1[CH:18]=[CH:17][CH:16]=[CH:15][CH:14]=1

참가 물질

6

실험 절차

The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate obtained in Example (160a) (100 mg, 0.38 mmol), methyl 3-bromo-4-fluorobenzoate (264 mg, 1.13 mmol), palladium acetate (25.5 mg, 0.11 mmol), BINAP (141 mg, 0.23 mmol) and cesium carbonate (370 mg, 1.13 mmol), to obtain 97.4 mg of the title compound as a yellow oily substance. mass spectrum (ESI): m/z 417 (M+H)+.

출처 및 근거

ORD 기록
ord-255be12eceab457691cdb2f24f685f8f
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08536197B2

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