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Water → (R)-2-(3-bromo-4-cyanophenylamino)-3-(1H-indol-3-yl)propanamide
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-fluorobenzonitrile | HCID 118939 | — |
| 反応物 | D-tryptophanamide | HCID 688582 | — |
| 溶媒 | Dimethyl Sulfoxide | HCID 679 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | (R)-2-(3-bromo-4-cyanophenylamino)-3-(1H-indol-3-yl)propanamide | HCID 67514877 | 31.3% |
反応手順
A solution of 2-bromo-4-fluorobenzonitrile (160 mg, 0.800 mmol), (R)-2-amino-3-(1H-indol-3-yl)propanamide (164 mg, 0.807 mmol) and DIEA (0.300 mL, 1.72 mmol) in DMSO (3 mL) was stirred at 120 C for 18 h. Water and EtOAc were added. The organic phase was separated, dried over Na2SO4, concentrated in vacuo. The residue was purified by a silica gel column, which was eluted with 0-80% EtOAc in hexane to give (R)-2-(3-bromo-4-cyanophenylamino)-3-(1H-indol-3-yl)propanamide (96 mg)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08846928B2 |
| 出典データセット | uspto-grants-2014_09 |
| ORD ID | ord-f6dd40fcc41b4bd491314c2b0ffc951d |
| 出典メモ | uspto-grants-2014_09 |