4-(N-Boc-amino)piperidine → Methyl 3-[4-({[(1,1-dimethylethyl)oxy]carbonyl}amino)-1-piperidinyl]-2-[6-(methyloxy)-1,5-naphthyridin-4-yl]propanoate

HRID 15296

反応式

[CH3:1][O:2][C:3]1[N:4]=[C:5]2[C:10](=[CH:11][CH:12]=1)[N:9]=[CH:8][CH:7]=[C:6]2[C:13](=[CH2:18])[C:14]([O:16][CH3:17])=[O:15].[NH:19]1[CH2:24][CH2:23][CH:22]([NH:25][C:26](=[O:32])[O:27][C:28]([CH3:31])([CH3:30])[CH3:29])[CH2:21][CH2:20]1>CN(C=O)C.CN(C)C(=N)N(C)C>[CH3:31][C:28]([O:27][C:26]([NH:25][CH:22]1[CH2:21][CH2:20][N:19]([CH2:18][CH:13]([C:6]2[C:5]3[C:10](=[CH:11][CH:12]=[C:3]([O:2][CH3:1])[N:4]=3)[N:9]=[CH:8][CH:7]=2)[C:14]([O:16][CH3:17])=[O:15])[CH2:24][CH2:23]1)=[O:32])([CH3:29])[CH3:30]

参加物

反応条件

温度: 70 °C

実験手順

To a solution of methyl 2-[6-(methyloxy)-1,5-naphthyridin-4-yl]-2-propenoate (2.53 g, 10.37 mmol) in DMF (4 ml) and tetramethylguanidine (0.1 ml) was added 1,1-dimethylethyl 4-piperidinylcarbamate (2.08 g, 10.37 mmol). The reaction was stirred for 1 hour at 70° C. after which time the solvent was evaporated. The residue was chromatographed on silica eluting with a gradient of 5% methanol in dichloromethane affording the desired compound as a yellow solid (2.66 g, 58%).

後処理

customwas evaporated
customThe residue was chromatographed on silica eluting with a gradient of 5% methanol in dichloromethane affording the desired compound as a yellow solid (2.66 g, 58%)

出典と根拠

ORDレコード: ord-3cf1206945f44fc7be4f7d9f075c1ab8
出典データセット: uspto-grants-2010_06
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07732461B2

反応式

参加物

反応物 2

生成物 1

試薬・触媒・溶媒 2

反応条件

実験手順

後処理

出典と根拠

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