関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 2-(1-(3-Fluoro-4-nitrobenzyl)piperidin-4-yl)propan-2-ol | HCID 60195822 | — |
| 反応物 | HCID 178511567 | HCID 178511567 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | HCID 178458679 | HCID 178458679 | 99% |
反応手順
To a suspension of trans-4-aminocyclohexanecarboxylic acid (0.199 g, 1.392 mmol) and DIPEA (0.553 mL, 3.16 mmol) in ACN (5 mL) was added 2-(1-(3-fluoro-4-nitrobenzyl)piperidin-4-yl)propan-2-ol (0.375 g, 1.265 mmol). The reaction was stirred at 75° C. After 48 hours, the reaction mixture was concentrated, diluted with water (10 mL) and extracted with DCM and EtOAc. The combined organic layers were dried over anhydrous magnesium sulfate, filtered, and concentrated to provide trans-4-(5-((4-(2-hydroxypropan-2-yl)piperidin-1-yl)methyl)-2-nitrophenylamino)cyclohexanecarboxylic acid (0.524 g, 1.249 mmol, 99% yield) as an orange powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09115127B2 |
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| 出典データセット | uspto-grants-2015_08 |
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| ORD ID | ord-10ba22e995374818b790ed327d8505c8 |
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| 出典メモ | uspto-grants-2015_08 |
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