참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Phenylpropanolamine | HCID 10297 | — |
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 5-iodo-1-isopropyl-1H-indazole | HCID 59339864 | — |
| 촉매 | Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI) | HCID 24350 | — |
| 용매 | Butyronitrile | HCID 8008 | — |
| 생성물 | (1R,2S)-1-[(1-isopropyl-1H-indazol-5-yl)oxy]-1-phenylpropan-2-amine | HCID 59339639 | — |
반응 단계
A mixture of 5-iodo-1-isopropyl-1H-indazole (129c, 461 mg, 1.26 mmol), (1R,2S)-2-amino-1-phenylpropan-1-ol (286 mg, 1.89 mmol), copper (I) iodide (25 mg, 130 μmol), and cesium carbonate (1.45 g, 3.8 mmol) in butyronitrile (5 ml) was stirred at 125° C. for 2 h. Then the mixture was cooled to r.t., the inorganic material was removed by filtration and washed with ethyl acetete. The combined organic solutions were concentrated in vacuo, and the product purified by flash chromatography on silica gel (ethyl acetate/methanol). Yield 200 mg (51%) of a brown oil.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07728030B2 |
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| 출처 데이터셋 | uspto-grants-2010_06 |
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| ORD ID | ord-36e1dcf13e4e41959da051f6f8d727ca |
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| 출처 메모 | uspto-grants-2010_06 |
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