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

HRID 43766

反応式

HRID 43766 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]([CH3:28])[N:25]=[C:24]([C:29]([O:31][CH2:32]C)=[O:30])[CH: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]([CH3:28])[N:25]=[C:24]([C:29]([O:31][CH3:32])=[O:30])[CH: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) (409 mg, 1.36 mmol), ethyl 4-chloro-6-methylpyridine-2-carboxylate (272 mg, 1.36 mmol), palladium acetate (30.6 mg, 0.14 mmol), BINAP (169 mg, 0.27 mmol) and cesium carbonate (1.33 g, 4.08 mmol), to obtain 194 mg of the title compound as a yellow oily substance.

出典と根拠

ORDレコード
ord-9241cb554be5495b89f0154e89f1cb91
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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