関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 2-Aminopyridine-4-carboxylic acid | HCID 278396 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | HCID 178493860 | HCID 178493860 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | HCID 178493855 | HCID 178493855 | 37.2% |
反応手順
7-Methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-amine (100 mg, 0.28 mol) was dissolved in DMF (3 mL), and 2-aminopyridine-4-carboxylic acid (38 mg, 0.28 mmol) was added. PYBOP (217 mg, 0.42 mmol) and diisopropylethylamine (0.15 mL, 0.83 mmol) were subsequently added, and the mixture was stirred at rt overnight. The mixture was purified by HPLC to give the title compound (50 mg, 37%). LC MS RT=1.02 min, MH+=480.3. 1H NMR (DMSO-d6) δ: 13.25 (1H, br s), 10.15 (1H, br s), 8.42 (1H, br s), 8.08 (1H, s), 8.06 (1H, d), 7.43 (1H, d), 7.75 (1H, s), 7.50 (1H, d), 7.38 (1H, dd), 4.50 (2H, dd), 4.35 (2H, br t), 4.27 (2H, dd), 4.01 (3H, s), 3.99 (2H, br s), 3.66 (2H, t), 3.50 (2H, d), 3.31 (2H, br t), 3.13 (2H, m), 2.25 (2H, m).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08466283B2 |
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| 出典データセット | uspto-grants-2013_06 |
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| ORD ID | ord-1b09de3ca90845aeb5718273284f3179 |
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| 出典メモ | uspto-grants-2013_06 |
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