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HRID 80619作成日:2026年10月26日

Cesium carbonate → (8S)-9-(3,5-difluorobenzyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one

https://huagongshe.com/reaction/80619

反応式

関与物質

役割名称HCID仕込み量
反応物Cesium carbonateHCID 10796—
反応物3,5-Difluorobenzyl bromideHCID 518896—
反応物(S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-oneHCID 136238743—
溶媒DimethylformamideHCID 6228—
生成物(8S)-9-(3,5-difluorobenzyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-oneHCID 49854298—

反応手順

The product is prepared according to the procedure described in Example 22, using 100 mg of (8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e), 214 mg of caesium carbonate and 75 mg of 1-(bromomethyl)-3,5-difluorobenzene in 2 ml of dimethylformamide. After purification by preparative HPLC/MS (Method C), 85 mg of (8S)-9-(3,5-difluorobenzyl)-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 an oil, the characteristics of which are the following:

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08846670B2
出典データセットuspto-grants-2014_09
ORD IDord-30376f3ba76943e08dd4d09acad6eb31
出典メモuspto-grants-2014_09