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Water → (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-phenylpropanamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (2R)-2-amino-3-phenylpropanamide | HCID 7000171 | — |
| 反応物 | 3,5-Dichloropyrazine-2-carbonitrile | HCID 52987744 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-phenylpropanamide | HCID 86685588 | 85.9% |
反応手順
A solution of 3,5-dichloropyrazine-2-carbonitrile (86 mg, 0.494 mmol), D-phenylalaninamide (81 mg, 0.494 mmol) and DIEA (0.130 mL, 0.747 mmol) in DMF (2 mL) was stirred at room temperature for 20 h. Water and EtOAc were added. Organic phase was separated, washed with 1N HCl, then with 5% NaHCO3, dried over Na2SO4, concentrated in vacuo to give (R)-2-(6-chloro-5-cyanopyrazin-2-ylamino)-3-phenylpropanamide (128 mg) as an oil.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09359308B2 |
| 出典データセット | uspto-grants-2016_06 |
| ORD ID | ord-2957b1622d0d4f708d953c960f099df7 |
| 出典メモ | uspto-grants-2016_06 |