関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 1H-Indazol-6-amine | HCID 81423 | — |
| 反応物 | Methyl 2,6-dichloro-4-cyanonicotinate | HCID 58317683 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | Methyl 2-(1H-indazol-6-ylamino)-6-chloro-4-cyanonicotinate | HCID 58317650 | 38.5% |
反応手順
A mixture of methyl 2,6-dichloro-4-cyanonicotinate (250 mg, 1.082 mmol), 1H-indazol-6-amine (173 mg, 1.299 mmol) and Et3N (0.226 mL, 1.623 mmol) in THF (10 mL) was stirred at 80° C. overnight. Water and EtOAc were added to the mixture. The organic phase was washed with H2O and brine, dried over MgSO4, and evaporated. The residue was purified by chromatography on SiO2(Hexane/EtOAc=5/1) to give the title compound as a yellow solid (120 mg, 38.5%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US08440689B2 |
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| 出典データセット | uspto-grants-2013_05 |
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| ORD ID | ord-55fcaf87709e40f2b4efbd4f4882cff3 |
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| 出典メモ | uspto-grants-2013_05 |
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