Cesium carbonate → HCID 59786580、化合物

HRID 1661481

反応式

HRID 1661481 の反応式
I[C:2]1[CH:3]=[C:4]2[C:8](=[CH:9][CH:10]=1)[N:7]([C:11]1[CH:12]=[N:13][CH:14]=[CH:15][CH:16]=1)[N:6]=[CH:5]2.[NH2:17][CH:18]([CH3:29])[CH:19]([C:21]1[CH:22]=[N:23][C:24]([O:27][CH3:28])=[CH:25][CH:26]=1)[OH:20].C(=O)([O-])[O-].[Cs+].[Cs+]>C(#N)CCC.C1(C)C=CC=CC=1.[Cu]I>[CH3:28][O:27][C:24]1[N:23]=[CH:22][C:21]([CH:19]([O:20][C:2]2[CH:3]=[C:4]3[C:8](=[CH:9][CH:10]=2)[N:7]([C:11]2[CH:12]=[N:13][CH:14]=[CH:15][CH:16]=2)[N:6]=[CH:5]3)[CH:18]([NH2:17])[CH3:29])=[CH:26][CH:25]=1

参加物

7

反応物 3

HCID 10796Cesium carbonateHCID 597865715-iodo-1-pyridin-3-yl-1H-indazoleHCID 59786583HCID 59786583、化合物

生成物 1

HCID 59786580HCID 59786580、化合物

試薬・触媒・溶媒 3

HCID 24350Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)触媒HCID 1140Toluene溶媒HCID 8008Butyronitrile溶媒

反応条件

温度
130 °C

実験手順

5-Iodo-1-(3-pyridinyl)indazole (750 mg, 2.3 mmole), 2-Amino-1-[6-methoxypyridin-3-yl]propan-1-ol (410 mg, 2.2 mmol), copper(I)iodide (42 mg, 0.22 mmol) and caesium carbonate (1.45 g, 4.5 mmole) were suspended in butyronitrile (2.4 mL) and toluene (4.8 mL). The reaction vessel was capped and the mixture was stirred at 130° C. for 20 hours. Then the solvent was removed i.vac., and the product purified by chromatography on silica gel. Yield 254 mg (3 0%) as a racemic mixture of two diastereomeres.

後処理

  1. customThe reaction vessel was capped
  2. customThen the solvent was removed i.vac
  3. custom, and the product purified by chromatography on silica gel
  4. additionYield 254 mg (3 0%) as a racemic mixture of two diastereomeres

出典と根拠

ORDレコード
ord-394ddf0596ae4f78ab2d49184cb624cf
出典データセット
uspto-grants-2011_10
特許番号
US08030340B2

関連ノート

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