2-氯乙醇 → 3-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2-hydroxyethyl)-piperidin-4-ylmethoxy]ethyl]-1H-indole-6-carboxamide

HRID 32429

反应方程式

HRID 32429 反应方程式
[Cl:1][C:2]1[C:10]2[C:5](=[CH:6][C:7]([C:11]([NH:13][CH:14]([C:24]3[CH:29]=[CH:28][CH:27]=[CH:26][C:25]=3[Cl:30])[CH2:15][O:16][CH2:17][CH:18]3[CH2:23][CH2:22][NH:21][CH2:20][CH2:19]3)=[O:12])=[CH:8][CH:9]=2)[NH:4][CH:3]=1.C(=O)([O-])[O-].[K+].[K+].[I-].[K+].Cl[CH2:40][CH2:41][OH:42]>CCO.O>[Cl:1][C:2]1[C:10]2[C:5](=[CH:6][C:7]([C:11]([NH:13][CH:14]([C:24]3[CH:29]=[CH:28][CH:27]=[CH:26][C:25]=3[Cl:30])[CH2:15][O:16][CH2:17][CH:18]3[CH2:23][CH2:22][N:21]([CH2:40][CH2:41][OH:42])[CH2:20][CH2:19]3)=[O:12])=[CH:8][CH:9]=2)[NH:4][CH:3]=1

参与物

7

反应物 4

HCID 342-氯乙醇HCID 4875碘化钾HCID 11430碳酸钾HCID 693078883-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide

产物 1

HCID 693105593-Chloro-N-[1-(2-chlorophenyl)-2-[1-(2-hydroxyethyl)-piperidin-4-ylmethoxy]ethyl]-1H-indole-6-carboxamide收率 32%

试剂、催化剂与溶剂 2

HCID 702乙醇溶剂HCID 962聚[6-[4-(4-氰基苯基)苯氧基]己基甲基丙烯酸酯]溶剂

实验过程

To a solution of 3-chloro-N-[1-(2-chlorophenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide (200 mg, 0.45 mmol) in 5 mL of EtOH was added potassium carbonate (247 mg, 1.8 mmol), potassium iodide (224 mg, 1.4 mmol) and 2-chloroethanol (0.09 mL, 1.4 mmol). The reaction was allowed to stir at room temperature overnight after which time water was added and the resulting precipitate was isolated by filtration. Purification of the filtrate (SiO2: 10:0.5 EtOAc:isopropylamine) provided 70 mg (32%) of the title compound.

后处理

  1. additionwas added
  2. customthe resulting precipitate was isolated by filtration
  3. customPurification of the filtrate (SiO2: 10:0.5 EtOAc:isopropylamine)

来源与证据

ORD记录
ord-820aeae5bdb84ba49a24b28cd989f7d3
来源数据集
uspto-grants-2008_09
专利号
US07427632B2

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