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HRID 81413作成日：2026年10月23日
4-Aminopyridine → 2-(biphenyl-4-ylmethyl)-7-isobutyl-5-methyl-3-(pyridin-4-ylamino)-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione
https://huagongshe.com/ja/reaction/81413
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 4-Aminopyridine | HCID 1727 | — |
| 反応物 | 1,1'-(9,9-Dimethyl-9H-xanthene-4,5-diyl)bis(1,1-diphenylphosphine) | HCID 636044 | — |
| 反応物 | 2-(biphenyl-4-ylmethyl)-3-iodo-7-isobutyl-5-methyl-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione | HCID 68505064 | — |
| 反応物 | HCID 178418922 | HCID 178418922 | — |
| 触媒 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 生成物 | 2-(biphenyl-4-ylmethyl)-7-isobutyl-5-methyl-3-(pyridin-4-ylamino)-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione | HCID 42640885 | — |
反応手順
2-(biphenyl-4-ylmethyl)-3-iodo-7-isobutyl-5-methyl-2H-pyrazolo[3,4-d]pyrimidine-4,6(5H,7H)-dione (13.6 mg, 0.026 mmol) is dissolved in anhydrous and degassed THF, and then 4-pyridyl amine (13 mg, 0.132 mmol), Pd2(dba)3 (12 mg, 0.013 mmol) and Xantphos (9 mg, 0.016 mmol) are added, followed by tBuOK (7.5 mg, 0.065 mmol). The reaction mixture is heated in microwave at 150° C. for 40 minutes. After cooling and filtration, the filtrate is purified by a semi-preparative HPLC to give product. MS (ESI) m/z 481.2 [M+H]+
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08846693B2 |
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| 出典データセット | uspto-grants-2014_09 |
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| ORD ID | ord-5074a99527b24e97a904d6d5ca7f3a40 |
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| 出典メモ | uspto-grants-2014_09 |
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