反応式
[F:1][CH:2]([F:18])[CH2:3][O:4][C@H:5]1[C@@H:10]([NH2:11])[CH2:9][CH2:8][N:7]([C:12](=[O:17])[C:13]([F:16])([F:15])[F:14])[CH2:6]1.[Cl:19][C:20]1[N:21]=[C:22]([C:27](O)=[O:28])[NH:23][C:24]=1[CH2:25][CH3:26].CCN=C=NCCCN(C)C.Cl.C1C=CC2N(O)N=NC=2C=1>ClCCl.CC(N(C)C)=O>[Cl:19][C:20]1[N:21]=[C:22]([C:27]([NH:11][C@H:10]2[CH2:9][CH2:8][N:7]([C:12](=[O:17])[C:13]([F:16])([F:14])[F:15])[CH2:6][C@H:5]2[O:4][CH2:3][CH:2]([F:1])[F:18])=[O:28])[NH:23][C:24]=1[CH2:25][CH3:26]参加物
7
反応物 4
生成物 1
試薬・触媒・溶媒 2
実験手順
The same operation as in Example (106d) was performed using cis(±)-3-(2,2-difluoroethoxy)-1-(trifluoroacetyl)piperidin-4-amine obtained in Example (121e) (0.79 g, 2.86 mmol), 4-chloro-5-ethyl-1H-imidazole 2-carboxylic acid (85% content, 0.62 g, 3 mmol), WSC hydrochloride (1.15 g, 6 mmol), HOBt (0.61 g, 4.5 mmol), DMA (15 mL) and dichloromethane (15 mL). The resulting residue was purified by silica gel column chromatography (elution solvent: ethyl acetate/hexane=1/4, 2/3, 3/2, 4/1) to obtain 0.82 g of the title compound as a colorless amorphous solid (63%).
後処理
- customThe resulting residue was purified by silica gel column chromatography (elution solvent: ethyl acetate/hexane=1/4, 2/3, 3/2, 4/1)
出典と根拠
- ORDレコード
- ord-11cd631c1fbd4d47b0af86e3b40d01cc
- 出典データセット
- uspto-grants-2015_01
- 特許番号
- US08927588B2
関連ノート
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