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Water → (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-3-cyclopropylpropanamide
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 | 2-Bromo-4,5-difluorobenzonitrile | HCID 19261277 | — |
| 反応物 | (R)-2-amino-3-cyclopropylpropanamide | HCID 59001002 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-3-cyclopropylpropanamide | HCID 67508107 | 99.9% |
反応手順
A solution of 2-bromo-4,5-difluorobenzonitrile (218 mg, 1.00 mmol), (R)-2-amino-3-cyclopropylpropanamide (188 mg, 1.14 mmol) and DIEA (0.600 mL, 3.45 mmol) in DMSO (3 mL) was stirred at 120 C for 18 h. Water and EtOAc were added. The organic phase was separated, washed with water, dried over Na2SO4, concentrated in vacuo to give (R)-2-(5-bromo-4-cyano-2-fluorophenylamino)-3-cyclopropylpropanamide (326 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09359375B2 |
| 出典データセット | uspto-grants-2016_06 |
| ORD ID | ord-6c434196f0eb473ca1c2169d53ac448e |
| 出典メモ | uspto-grants-2016_06 |