Propargyl bromide → HCID 59835761、化合物

HRID 1916716ノート

反応式

HRID 1916716 の反応式
C([O-])([O-])=O.[K+].[K+].Br[CH2:8][C:9]#[CH:10].[Cl:11][C:12]1[CH:17]=[CH:16][C:15]([C:18]2[CH:19]=[CH:20][C:21]([C:24]#[C:25][C:26]3[CH:27]=[C:28]4[C:32](=[CH:33][CH:34]=3)[N:31]([CH2:35][CH2:36][NH:37][CH2:38][CH:39]3[CH2:41][CH2:40]3)[CH:30]=[CH:29]4)=[N:22][CH:23]=2)=[CH:14][CH:13]=1>CN(C=O)C>[Cl:11][C:12]1[CH:13]=[CH:14][C:15]([C:18]2[CH:19]=[CH:20][C:21]([C:24]#[C:25][C:26]3[CH:27]=[C:28]4[C:32](=[CH:33][CH:34]=3)[N:31]([CH2:35][CH2:36][N:37]([CH2:38][CH:39]3[CH2:40][CH2:41]3)[CH2:10][C:9]#[CH:8])[CH:30]=[CH:29]4)=[N:22][CH:23]=2)=[CH:16][CH:17]=1

参加物

5

反応物 3

HCID 7842Propargyl bromideHCID 11430Potassium CarbonateHCID 59835834(2-{5-[5-(4-Chloro-phenyl)-pyridin-2-ylethynyl]-indol-1-yl}-ethyl)-cyclopropylmethyl-amine

生成物 1

HCID 59835761HCID 59835761、化合物

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

45 mg (0.33 mmol) K2CO3 and 13 μL (0.18 mmol) 3-bromo-propyne are added at RT to a solution of 70 mg (0.16 mmol) (2-{5-[5-(4-chloro-phenyl)-pyridin-2-ylethynyl]-indol-1-yl}-ethyl)-cyclopropylmethyl-amine in 2 mL DMF and the reaction mixture is stirred for 4 h at RT. The mixture is evaporated down i. vac., the residue is taken up in water, extracted exhaustively with DCM and the organic phase is dried over Na2SO4. After the desiccant and solvent have been eliminated the residue is purified by chromatography (Alox, cyc/EtOAc 4:1).

後処理

  1. customThe mixture is evaporated down i
  2. extractionextracted exhaustively with DCM
  3. dry with materialthe organic phase is dried over Na2SO4
  4. customis purified by chromatography (Alox, cyc/EtOAc 4:1)

出典と根拠

ORDレコード
ord-c6a03cbd963240678ee8fb810c8f1717
出典データセット
uspto-grants-2013_12
特許番号
US08618132B2

反応ノート

読み込み中…