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HRID 32654作成日：2026年10月25日
4-Bromo-3-fluorobenzotrifluoride → 4-(2-Fluoro-4-trifluoromethylphenyl)piperazine-1-carboxylic acid tert-butyl ester
https://huagongshe.com/reaction/32654
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Bromo-3-fluorobenzotrifluoride | HCID 142414 | — |
| 反応物 | tert-Butyl piperazine-1-carboxylate | HCID 143452 | — |
| 反応物 | 2-(Dicyclohexylphosphino)biphenyl | HCID 2734216 | — |
| 触媒 | Palladium, tris[mu-[(1,2-eta:4,5-eta)-(1E,4E)-1,5-diphenyl-1,4-pentadien-3-one]]di-, compd. with trichloromethane (1:1) | HCID 11029508 | — |
| 溶媒 | Toluene | HCID 1140 | — |
| 生成物 | 4-(2-Fluoro-4-trifluoromethylphenyl)piperazine-1-carboxylic acid tert-butyl ester | HCID 53485517 | — |
反応手順
A mixture of 5 g (20 mmol) 1-Bromo-2-fluoro-4-trifluoromethyl-benzene, 4.6 g (24.7 mmol) n-Boc-piperazine, 106 mg (0.1 mmol) Tris(dibenzylideneacetone)dipalladium chloroform complex 2.77 g (28.8 mmol) sodium-t-butoxide and 144 mg (0.4 mmol) 2-(Dicyclohexylphosphino)biphenyl in 50 ml toluene was heated for 16 h at 80° C. After cooling to room temperature the mixture was treated with 15 g Isolute HM-N and all volatiles were removed under vacuum. The residue was purified on silica eluting with a gradient of heptane/EtOAc to yield after evaporation 4.54 g (63%) of the title compound as white amorphous solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07427612B2 |
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| 出典データセット | uspto-grants-2008_09 |
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| ORD ID | ord-177df3555d644298b3f65361ea2c9a5f |
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| 出典メモ | uspto-grants-2008_09 |
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