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Morpholine → (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Morpholine | HCID 8083 | — |
| 反応物 | (S)-8-chloro-2-(trifluoromethyl)-3,4-dihydro-1H-pyrimido[1,2-a]pyrimidin-6(2H)-one | HCID 136238740 | — |
| 生成物 | (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one | HCID 136238743 | — |
反応手順
A mixture of 1 g of (S)-2-chloro-8-trifluoromethyl-6,7,8,9-tetrahydro-pyrimido[1,2-a]pyrimidin-4-one and of 15 ml of morpholine is heated at 80° C. After one and a half hours of heating and after verification by LC/MS, the reaction is complete. After cooling, the reaction mixture is concentrated under reduced pressure. 10 ml of cold water and 100 ml of ethyl acetate are added to the residue obtained. The resulting organic phase is separated and then dried over magnesium sulphate, filtered, and concentrated under reduced pressure so as to give 1.2 g of (S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one, 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 |
| 出典データセット | uspto-grants-2014_09 |
| ORD ID | ord-98dcb3b1368642d2a805e9acb940d9a4 |
| 出典メモ | uspto-grants-2014_09 |