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3-Fluorobenzylamine → N-(3-Fluoro-benzyl)-2-(2-fluoro-biphenyl-4-yl)-acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Fluorobenzylamine | HCID 66853 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | 2-(2-Fluoro-(1,1'-biphenyl)-4-yl)acetic acid | HCID 11831237 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-(3-Fluoro-benzyl)-2-(2-fluoro-biphenyl-4-yl)-acetamide | HCID 11580859 | — |
反応手順
(2-Fluoro-biphenyl-4-yl)-acetic acid (0.12 gm, 0.5 mmole), 3-fluorobenzylamine (0.0.8 ml, 0.6 mmole), PyBOP (0.34 gm, 0.6 mmole), and DIEA (0.22 ml, 1.3 mmole) was dissolved in DMF stirred overnight, the reaction mixture was then poured into water, solid was collected by filtration, re-crystallized using water-methanol. (0.140 gm, 83%); H1-NMR INOVA-500 (DMSO d6) δ 3.580 (s, 2H), 4.316 (d, J=5.5 Hz, 2H), 7.037-7.110 (m, 3H), 7.210-7.247 (m, 2H), 7.343-7.372 (m, 2H), 7.457-7.501 (m, 3H), 7.544 (d, J=8.0 Hz, 2H), 8.660 (t, J=6.0 Hz, 1H). MS (m/z) 338.1 (M+H)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08980890B2 |
| 出典データセット | uspto-grants-2015_03 |
| ORD ID | ord-0aa7510f7150490ba13afec69d9afa19 |
| 出典メモ | uspto-grants-2015_03 |