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Diisopropylethylamine → tert-butyl (3R,4R)-4-(6-chloro-5-cyanopyrazin-2-ylamino)tetrahydro-2H-pyran-3-ylcarbamate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 3,5-Dichloropyrazine-2-carbonitrile | HCID 52987744 | — |
| 反応物 | tert-Butyl ((3R,4R)-4-aminotetrahydro-2H-pyran-3-yl)carbamate | HCID 68077633 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 溶媒 | 2-Oxopropiononitrile | HCID 69430 | — |
| 生成物 | tert-butyl (3R,4R)-4-(6-chloro-5-cyanopyrazin-2-ylamino)tetrahydro-2H-pyran-3-ylcarbamate | HCID 86685613 | 119% |
反応手順
To a mixture of 3,5-dichloropyrazine-2-carbonitrile (369 mg, 2.09 mmol) and tert-butyl (3R,4R)-4-aminotetrahydro-2H-pyran-3-ylcarbamate (500 mg, 2.3 mmol) in AcCN (7.5 mL) was added DIPEA (0.41 mL, 2.3 mmol). After stirring at room temperature for 5 h, it was diluted with EtOAc, washed with sat. NaHCO3, organic layer was separated and washed with brine, dried and concentrated to give tert-butyl (3R,4R)-4-(6-chloro-5-cyanopyrazin-2-ylamino)tetrahydro-2H-pyran-3-ylcarbamate (880 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08877760B2 |
| 出典データセット | uspto-grants-2014_11 |
| ORD ID | ord-9bbb4225545947a8975319ccc4033376 |
| 出典メモ | uspto-grants-2014_11 |