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1,4-Bis(dihydroquinidine)phthalazine → (R)-4-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)but-3-yne-1,2-diol
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1,4-Bis(dihydroquinidine)phthalazine | HCID 11217202 | — |
| 反応物 | t-Butanol tetrahydrofuran water | HCID 22124471 | — |
| 反応物 | 5-(but-3-en-1-ynyl)-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-2-amine | HCID 57713813 | — |
| 生成物 | (R)-4-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)but-3-yne-1,2-diol | HCID 57713808 | — |
反応手順
Treatment of 5-(but-3-en-1-ynyl)-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-2-amine (see example 46) (35 mg) with AD-mix-β (Aldrich, 540 mg) in t-BuOH:THF:water 1:1:1 (6 mL) at rt overnight, followed by work-up and reverse-phase preparative HPLC gave the title compound (10 mg), as a solid. HPLC Rt=4.13 min
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08093229B2 |
| 出典データセット | uspto-grants-2012_01 |
| ORD ID | ord-4e185b1b4b5245d894c17f88949288b9 |
| 出典メモ | uspto-grants-2012_01 |