Cesium carbonate → HCID 59786580, 화합물

HRID 1661481노트

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HRID 1661481 반응식
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

참가 물질

7

반응물 3

HCID 10796Cesium carbonateHCID 597865715-iodo-1-pyridin-3-yl-1H-indazoleHCID 59786583HCID 59786583, 화합물

생성물 1

HCID 59786580HCID 59786580, 화합물

시약·촉매·용매 3

HCID 24350Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)촉매HCID 1140Toluene용매HCID 8008Butyronitrile용매

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온도
130 °C

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-394ddf0596ae4f78ab2d49184cb624cf
출처 데이터셋
uspto-grants-2011_10
특허 번호
US08030340B2

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