Cesium carbonate → Methyl cis(+/-)-2-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-6-methylpyridine-4-carboxylate

HRID 43762

反応式

HRID 43762 の反応式
Cl.[CH3:2][O:3][C@H:4]1[C@@H:9]([NH:10][C:11](=[O:20])[O:12][CH2:13][C:14]2[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=2)[CH2:8][CH2:7][NH:6][CH2:5]1.Cl[C:22]1[CH:27]=[C:26]([C:28]([O:30][CH3:31])=[O:29])[CH:25]=[C:24]([CH3:32])[N:23]=1.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>[CH2:13]([O:12][C:11]([NH:10][C@H:9]1[CH2:8][CH2:7][N:6]([C:22]2[CH:27]=[C:26]([C:28]([O:30][CH3:31])=[O:29])[CH:25]=[C:24]([CH3:32])[N:23]=2)[CH2:5][C@H:4]1[O:3][CH3:2])=[O:20])[C:14]1[CH:19]=[CH:18][CH:17]=[CH:16][CH:15]=1

参加物

6

実験手順

The same operation as in Example (42a) was performed using benzyl cis(±)-[3-methoxypiperidin-4-yl]carbamate hydrochloride obtained in Example (160a) (384 mg, 1.45 mmol), methyl 2-chloro-6-methylpyridine-4-carboxylate (243 mg, 1.31 mmol), palladium acetate (32.7 mg, 0.15 mmol), BINAP (181 mg, 0.29 mmol) and cesium carbonate (1.42 g, 4.36 mmol), to obtain 40.1 mg of the title compound as a yellow oily substance (6.7%).

出典と根拠

ORDレコード
ord-07df82e89cf24c2d836442d94e64ad27
出典データセット
uspto-grants-2013_09
特許番号
US08536197B2

関連ノート

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