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Boron tribromide → 4-{5(Cyclopentylamino)-3-[2-(cyclopentylamino)-4-pyrimidinyl]pyrazolo[1,5-alpha]pyridin-2yl}phenol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Boron tribromide | HCID 25134 | — |
| 反応物 | N-cyclopentyl-3-[2-(cyclopentylamino)-4-pyrimidinyl]-2-(4-methoxyphenyl)-pyrazolo[1,5-alpha]pyridin-5-amine | HCID 9847463 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 4-{5(Cyclopentylamino)-3-[2-(cyclopentylamino)-4-pyrimidinyl]pyrazolo[1,5-alpha]pyridin-2yl}phenol | HCID 135452830 | 81% |
反応手順
Treatment of N-cyclopentyl-3-[2-(cyclopentylamino)-4-pyrimidinyl]-2-(4-methoxyphenyl)pyrazolo[1,5-α]pyridin-5-amine (500 mg, 1.07 mmol) in dichloromethane with boron tribromide, followed by aqueous workup, gave 4-{5-(cyclopentylamino)-3-[2-(cyclopentylamino)-4-pyrimidinyl]pyrazolo[1,5-α]pyridin-2-yl}phenol (390 mg, 81%) as a yellow solid. 1H NMR (CD3OD) δ 8.16 (d, 1H), 7.85 (d, 1H), 7.40 (m, 3H), 6.90 (d, 2H), 6.53 (dd, 1H), 6.27 (d, 1H), 4.44 (m, 1H), 3.92 (m, 1H), 2.11 (m, 4H), 1.84–1.58 (m, 12H). MS m/z 455 (M+1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07141569B2 |
| 出典データセット | uspto-grants-2006_11 |
| ORD ID | ord-0cbeefeec8f74fdf9502e4f1dd834d54 |
| 出典メモ | uspto-grants-2006_11 |