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Chlorotrimethylsilane → 6-(4-(1-methyl-1H-indazol-5-ylamino)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Chlorotrimethylsilane | HCID 6397 | — |
| 反応物 | 6-amino-3,4-dihydroquinolin-2(1H)-one | HCID 4912759 | — |
| 反応物 | 2-chloro-N-(1-methyl-1H-indazol-5-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine | HCID 86628043 | — |
| 溶媒 | 1-Butanol | HCID 263 | — |
| 生成物 | 6-(4-(1-methyl-1H-indazol-5-ylamino)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one | HCID 68579389 | 12.4% |
反応手順
A mixture of 2-chloro-N-(1-methyl-1H-indazol-5-yl)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-4-amine (1158 mg, 0.349 mmol), 6-amino-3,4-dihydroquinolin-2(1H)-one (113 mg, 0.697 mmol) and TMSCl (0.300 mL, 2.37 mmol) in nBuOH (3 mL) was stirred at 135° C. for 44 h. nBuOH was removed in vacuo. The residue was purified by HPLC to give 6-(4-(1-methyl-1H-indazol-5-ylamino)-7-tosyl-7H-pyrrolo[2,3-d]pyrimidin-2-ylamino)-3,4-dihydroquinolin-2(1H)-one (25 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07705004B2 |
| 出典データセット | uspto-grants-2010_04 |
| ORD ID | ord-46fc3217643f4b1190fa2873dcf27c1d |
| 出典メモ | uspto-grants-2010_04 |