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2-(4-Tert-butylphenoxy)acetic acid → 2-[2-(4-Tert-butyl-phenoxy)-acetylamino]-isonicotinamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-(4-Tert-butylphenoxy)acetic acid | HCID 15718 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 2-Aminoisonicotinamide | HCID 351653 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 2-[2-(4-Tert-butyl-phenoxy)-acetylamino]-isonicotinamide | HCID 44218653 | 56.5% |
反応手順
A solution of 4-tert-butylphenoxy acetic acid (60.1 mg, 0.29 mmol), 2-amino isonicotinamide (60.3 mg, 0.44 mmol), DIPEA (0.1 ml, 0.58 mmol) and PyBOP (301.8 mg, 0.58 mmol) in DMF 4.0 mL was stirred, then partitioned between ethyl acetate and water. The organic phase was washed with brine, dried over anhydrous MgSO4, and concentrated. The residue was purified by Prep-TLC (n-Hexane:EtoAc:MeOH=6:3:1) to give 2-[2-(4-tert-butyl-phenoxy)-acetylamino]-isonicotinamide as a white solid (53.6 mg, 56.5% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08394799B2 |
| 出典データセット | uspto-grants-2013_03 |
| ORD ID | ord-a0d3027d71c24f2ea89ebae75ab096c4 |
| 出典メモ | uspto-grants-2013_03 |