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6-chloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purine → 8-Methyl-3-((methyl(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-yl)amino)methyl)-2-o-tolylisoquinolin-1(2H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 6-chloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purine | HCID 97740 | — |
| 反応物 | 8-Methyl-3-((methylamino)methyl)-2-o-tolylisoquinolin-1(2H)-one | HCID 58008619 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | 8-Methyl-3-((methyl(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-yl)amino)methyl)-2-o-tolylisoquinolin-1(2H)-one | HCID 58008570 | 51% |
反応手順
8-Methyl-3-((methylamino)methyl)-2-o-tolylisoquinolin-1(2H)-one (233 mg, 0.8 mmol) (4001) and 6-chloro-9-(tetrahydro-2H-pyran-2-yl)-9H-purine (4002) (238 mg, 1.0 mmol) were dissolved in EtOH (50 mL) and the resulting mixture was stirred at reflux for 2 h. The mixture was allowed to cool to RT, and concentrated in vacuo. The residue was purified by flash column chromatography on silica gel (2-20% MeOH/DCM) to afford the product, 8-Methyl-3-((methyl(9-(tetrahydro-2H-pyran-2-yl)-9H-purin-6-yl)amino)methyl)-2-o-tolylisoquinolin-1(2H)-one (4003) (200 mg, 51% yield) as a slight yellow solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09206182B2 |
| 出典データセット | uspto-grants-2015_12 |
| ORD ID | ord-85778f8a6d2d40dc871ef02610627896 |
| 出典メモ | uspto-grants-2015_12 |