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2-(Oxan-4-yl)ethan-1-amine → 5-(2-Fluoro-4-{[2-(tetrahydropyran-4-yl)ethylamino]methyl}phenoxy)pyridine-2-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-(Oxan-4-yl)ethan-1-amine | HCID 2773198 | — |
| 反応物 | 5-(2-Fluoro-4-formylphenoxy)pyridine-2-carboxamide | HCID 59729937 | — |
| 生成物 | 5-(2-Fluoro-4-{[2-(tetrahydropyran-4-yl)ethylamino]methyl}phenoxy)pyridine-2-carboxamide | HCID 59730156 | 44.3% |
反応手順
Using a method similar to Example 405, a reaction of 5-(2-fluoro-4-formylphenoxy)pyridine-2-carboxamide (Example 403, Part B) (0.0294 g, 0.113 mmol) and 2-(tetrahydropyran-4-yl)ethylamine (0.016 g, 0.124 mmol) gives the title compound (0.0187 g 44.2%): TOF MS ES+ 374.2 (M+H)+, HRMS calcd for C20H25N3O3F 374.1880 (M+H)+, found 374.1863, time 0.39 min; HPLC [YMC-Pack Pro C-18 (150×4.6 mm, S-5 microm), 0.1% TFA/acetonitrile in 0.1% TFA/water at 1.0 mL/min, 30-99% over 19 min], tR=5.2 min, 95.2% purity.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07381719B2 |
| 出典データセット | uspto-grants-2008_06 |
| ORD ID | ord-b70b7905d32d4fd7ab20dfa88fd56e14 |
| 出典メモ | uspto-grants-2008_06 |