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HRID 2067908作成日：2026年10月26日
Methyl isonipecotate → Methyl 1-(2-(5-(5-bromopyrimidin-2-ylamino)-2-fluorophenoxy)ethyl)piperidine-4-carboxylate
https://huagongshe.com/reaction/2067908
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Methyl isonipecotate | HCID 424914 | — |
| 反応物 | 2-(5-(5-Bromopyrimidin-2-ylamino)-2-fluorophenoxy)ethyl methanesulfonate | HCID 86660123 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 生成物 | Methyl 1-(2-(5-(5-bromopyrimidin-2-ylamino)-2-fluorophenoxy)ethyl)piperidine-4-carboxylate | HCID 58542307 | — |
反応手順
2-(5-(5-bromopyrimidin-2-ylamino)-2-fluorophenoxy)ethyl methanesulfonate 46b (0.24 mmol) and methyl piperidine-4-carboxylate (0.48 mmol) are dissolved in NMP (2 mL) and heated to 90° C. for 3 h. The reaction mixture is cooled to rt and diluted with water and extracted with EtOAc (2×30 mL). The organic layer is washed with water, brine, dried over sodium sulfate, and concentrated to dryness. The crude product is purified by short SiO2 chromatography using DCM:hexane=9:1 as eluant to yield methyl 1-(2-(5-(5-bromopyrimidin-2-ylamino)-2-fluorophenoxy)ethyl)piperidine-4-carboxylate 47 as light brown solid. MS (m/z) (M+1)+: 454.1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08293757B2 |
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| 出典データセット | uspto-grants-2012_10 |
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| ORD ID | ord-5eacd9c8f44141448122ab8b1c12f878 |
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| 出典メモ | uspto-grants-2012_10 |
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