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HRID 80623作成日：2026年10月26日
3-Iodotoluene → (8S)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one
https://huagongshe.com/reaction/80623
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 3-Iodotoluene | HCID 12268 | — |
| 反応物 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 反応物 | 1,2-Diaminocyclohexane, (+)- | HCID 479307 | — |
| 反応物 | (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one | HCID 136238743 | — |
| 触媒 | Copper iodide | HCID 83717 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 溶媒 | Dichloromethane methanol | HCID 21226129 | — |
| 生成物 | (8S)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one | HCID 49854400 | — |
反応手順
The product is prepared according to the procedure described in Example 12, but using 250 mg of (8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 4 ml of dimethylformamide, 251 mg of 1-iodo-3-methylbenzene, 349 mg of tripotassium phosphate, 156 mg of copper iodide and 93 mg of (1S,2S)-cyclo-hexane-1,2-diamine. After 1 hour at 150° C. under microwave irradiation and silica column purification of the resulting reaction mixture (elution gradient of CH2Cl2 to CH2Cl2/MeOH 98/02), 195 mg of (88)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]-pyrimidin-4-one are obtained in the form of a green solid, the characteristics of which are the following:
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08846670B2 |
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| 出典データセット | uspto-grants-2014_09 |
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| ORD ID | ord-072e0694c5ce44418a2b16a7001210a6 |
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| 出典メモ | uspto-grants-2014_09 |
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