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HRID 1512006作成日:2026年10月26日
Ethyl 3-chloro-3-oxopropionate → 1-[(2-Ethoxycarbonyl-acetyl)-(4-fluoro-benzyl)-amino]-6-trifluoromethyl-1H-indole-2-carboxylic acid ethyl ester
https://huagongshe.com/reaction/1512006
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Ethyl 3-chloro-3-oxopropionate | HCID 118931 | — |
| 反応物 | 1-(4-fluoro-benzylamino)-6-trifluoromethyl-1H-indole-2-carboxylic acid ethyl ester | HCID 67230303 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 1-[(2-Ethoxycarbonyl-acetyl)-(4-fluoro-benzyl)-amino]-6-trifluoromethyl-1H-indole-2-carboxylic acid ethyl ester | HCID 67230480 | 52% |
反応手順
A mixture of 1-(4-fluoro-benzylamino)-6-trifluoromethyl-1H-indole-2-carboxylic acid ethyl ester (240 mg, 0.63 mmol) and chlorocarbonyl-acetic acid ethyl ester (105 mg, 0.69 mmol) in dioxane (3 mL) was heated in an 100° C. oil bath for 30 min and concentrated. Crude product was purified by silica gel chromatography (5%-50% EtOAc/DCM) to provide the title compound 162 mg. ESI (m/z): 495.24 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08217043B2 |
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| 出典データセット | uspto-grants-2012_07 |
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| ORD ID | ord-fc86f27af53942f48954e69854928e81 |
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| 出典メモ | uspto-grants-2012_07 |
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