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Aminopyrazine → N-pyrazin-2-yl-4-(3-{[5-(trifluoromethyl)pyridin-2-yl]oxy}benzylidene)piperidine-1-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Aminopyrazine | HCID 78747 | — |
| 反応物 | 2-(3-(Piperidin-4-ylidenemethyl)phenoxy)-5-(trifluoromethyl)pyridine hydrochloride | HCID 66876161 | — |
| 反応物 | Phenyl pyrazin-2-ylcarbamate | HCID 66876316 | — |
| 生成物 | N-pyrazin-2-yl-4-(3-{[5-(trifluoromethyl)pyridin-2-yl]oxy}benzylidene)piperidine-1-carboxamide | HCID 24967991 | — |
反応手順
Following the procedure in Example 1, Step 6, 2-(3-piperidin-4-ylidenemethyl-phenoxy)-5-trifluoromethyl-pyridine hydrochloride (150 mg, 0.40 mmol, from Example 1, Step 5) and phenyl pyrazin-2-ylcarbamate (261 mg, 1.2 mmol, prepared according to the procedure described in Synthesis, 1997, 1189-1194 from aminopyrazine) were used to provide the title compound (24 mg). MS (APCI 10V) AP+ 456.2, 376.2, 335.2, AP− 454.2, 435.1; 1H NMR (400 MHz, CD3OD) δ ppm 2.43-2.50 (m, 2H) 2.56-2.62 (m, 2H) 3.54-3.61 (m, 2H) 3.64-3.70 (m, 2H) 6.46 (s, 1H) 6.98-7.05 (m, 2H) 7.10-7.17 (m, 2H) 7.40 (td, J=7.72, 0.67 Hz, 1H) 8.06-8.11 (m, 1H) 8.16 (d, J=2.68 Hz, 1H) 8.28 (dd, J=2.68, 1.54 Hz, 1H) 8.43 (ddd, J=2.56, 1.71, 0.85 Hz, 1H) 9.04 (d, J=1.56 Hz, 1H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08044052B2 |
| 出典データセット | uspto-grants-2011_10 |
| ORD ID | ord-f26809a8a59c495aa199e1de8e974960 |
| 出典メモ | uspto-grants-2011_10 |