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HRID 920363作成日:2026年10月25日
Sodium hydride → 5-(((1-methyl-6-oxo-2,3,4,6-tetrahydro-1H-pyrimido[1,6-a]pyrimidin-8-yl)oxy)methyl)-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzonitrile
https://huagongshe.com/reaction/920363
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Sodium hydride | HCID 24758 | — |
| 反応物 | 5-(Hydroxymethyl)-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzonitrile | HCID 66825657 | — |
| 反応物 | 8-Chloro-1-methyl-3,4-dihydro-1H-pyrimido[1,6-A]pyrimidin-6(2H)-one | HCID 71743471 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 5-(((1-methyl-6-oxo-2,3,4,6-tetrahydro-1H-pyrimido[1,6-a]pyrimidin-8-yl)oxy)methyl)-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzonitrile | HCID 71236637 | — |
反応手順
The title compound was prepared by a procedure similar to that described for E1 starting from 8-chloro-1-methyl-3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one and 5-(hydroxymethyl)-2-5 ((5-(trifluoromethyl)pyridin-2-yl)oxy)benzonitrile. An exemplary process is shown as below: To a solution of 5-(hydroxymethyl)-2-((5-(trifluoromethyl)pyridin-2-yl)oxy)benzonitrile (0.108 mL, 0.601 mmol) in N,N-dimethylformamide (DMF) (5 mL) was added NaH (48.1 mg, 1.202 mmol) and stirred for 10 mins. Then 8-chloro-1-methyl-3,4-dihydro-1H-pyrimido[1,6-a]pyrimidin-6(2H)-one (80 mg, 0.401 mmol) was charged and stirred for 45 mins at rt. The resulting solution was 10 quenched by addition of 1 mL aq. NH4Cl and the solution was filtered. The resulting solution was submitted for MDAP to afford the desired product as a white solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US09273054B2 |
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| 出典データセット | uspto-grants-2016_03 |
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| ORD ID | ord-78e117bd89b24d3ea0196cf7218b9e19 |
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| 出典メモ | uspto-grants-2016_03 |
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