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Diisopropylethylamine → Methyl 2-(4-methyl-2-(piperidin-1-yl)-6-(2,4,5-trifluorophenyl)pyrimidin-5-yl)pentanoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 2,4,5-Trifluorophenylboronic acid | HCID 2783133 | — |
| 反応物 | Methyl 2-(4-chloro-6-methyl-2-(piperidin-1-yl)pyrimidin-5-yl)pentanoate | HCID 86665653 | — |
| 触媒 | Tetrakis(triphenylphosphine)palladium | HCID 11979704 | — |
| 溶媒 | Water 1,2-dimethoxyethane | HCID 18180031 | — |
| 生成物 | Methyl 2-(4-methyl-2-(piperidin-1-yl)-6-(2,4,5-trifluorophenyl)pyrimidin-5-yl)pentanoate | HCID 66955535 | 76% |
反応手順
This compound was prepared according to general method E from methyl 2-(4-chloro-6-methyl-2-(piperidin-1-yl)pyrimidin-5-yl)pentanoate (0.081 g; 0.25 mmol), tetrakis(triphenylphosphine) palladium(0) (0.029 g; 0.025 mmol), N,N-diisopropylethylamine (0.172 mL; 1.00 mmol) and 2,4,5-trifluorophenylboronic acid (0.088 g; 0.500 mmol) in DME-water (1 mL) for 20 min. Purification by flash-chromatography on silica gel using a gradient of ethyl acetate (1-10%) in heptane furnished 0.080 g (76%) of the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08906906B2 |
| 出典データセット | uspto-grants-2014_12 |
| ORD ID | ord-ee9120a35d6a4ce9b7926d219e52c9c2 |
| 出典メモ | uspto-grants-2014_12 |