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HRID 57602作成日：2026年10月27日
Cesium carbonate → (S)-tert-butyl 3-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate
https://huagongshe.com/reaction/57602
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | (4-(Morpholin-4-yl)phenyl)boronic acid | HCID 2795359 | — |
| 反応物 | (S)-tert-butyl 3-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate | HCID 86717378 | — |
| 触媒 | Palladium Chloride | HCID 24290 | — |
| 溶媒 | Dimethoxyethane ethanol | HCID 20074477 | — |
| 生成物 | (S)-tert-butyl 3-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate | HCID 71113712 | 73% |
反応手順
A mixture of (S)-tert-butyl 3-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate (0.15 mmol), 4-morpholinophenylboronic acid (0.23 mmol), PdCl2 (dppf) (0.015 mmol) and Cs2CO3 (0.30 mmol) in dimethoxyethane/ethanol was sealed in a microwave reaction and stirred at 160° C. for 45 minutes in a microwave reactor. The mixture was cooled to room temperature, concentrated, and purified by chromatography to afford the title compound (73% yield). MS (m/z): 505 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US09434726B2 |
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| 出典データセット | uspto-grants-2016_09 |
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| ORD ID | ord-059884758c924940b47b252436c2fba7 |
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| 出典メモ | uspto-grants-2016_09 |
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