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HRID 72382作成日:2026年10月25日

Cesium carbonate → (2S)-1-(3-Bromo-4-fluorobenzyl)-2-methyl-7-(morpholin-4-yl)-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one

https://huagongshe.com/reaction/72382

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-Bromo-4-fluorobenzyl BromideHCID 12922710—
反応物(2S)-2-methyl-7-morpholin-4-yl-2-trifluoromethyl-2,3-dihydro-1H-imidazo[1,2-a]pyrimidin-5-oneHCID 136069602—
生成物(2S)-1-(3-Bromo-4-fluorobenzyl)-2-methyl-7-(morpholin-4-yl)-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-oneHCID 50899613—

反応手順

The product is prepared according to the procedure described in stage k of Example 1, using 100 mg of (2S)-2-methyl-7-(morpholin-4-yl)-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one (Example 1j) and 106 mg of 2-bromo-4-(bromomethyl)-1-fluorobenzene, replacing the sodium hydride with 214 mg of caesium carbonate. After purification by preparative HPLC/MS (method C), 50 mg of (2S)-1-(3-bromo-4-fluorobenzyl)-2-methyl-7-(morpholin-4-yl)-2-(trifluoromethyl)-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)-one are obtained in the form of a off-white semi-solid, the characteristics of which are the following:

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08828997B2
出典データセットuspto-grants-2014_09
ORD IDord-e6211effa00640babff14b901e65f90c
出典メモuspto-grants-2014_09