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HRID 43392作成日:2026年10月23日

Water → 4-{5-[(4-{[4-(Trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]-2-pyridinyl}morpholine

https://huagongshe.com/ja/reaction/43392

反応式

関与物質

役割名称HCID仕込み量
反応物WaterHCID 962—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物DiisopropylethylamineHCID 81531—
反応物1-[4-(Trifluoromethyl)benzenesulfonyl]piperazineHCID 2554578—
反応物Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 2733084—
反応物6-Morpholinonicotinic AcidHCID 2776460—
溶媒DimethylformamideHCID 6228—
生成物4-{5-[(4-{[4-(Trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]-2-pyridinyl}morpholineHCID 2611210278.2%

反応手順

To a solution of 1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (Description 1) (80 mg, 0.272 mmol) in DMF (5 ml) were added 6-(4-morpholinyl)-3-pyridinecarboxylic acid (56.6 mg, 0.272 mmol), HOBT.H2O (41.6 mg, 0.272 mmol), HBTU (103 mg, 0.272 mmol) and DIPEA (0.142 ml, 0.816 mmol) and the reaction mixture was stirred at room temperature for 2 h. The DMF was evaporated in vacuo then 5 ml of DCM were added and washed with saturated aqueous NaHCO3 solution (5 ml), dried on a phase separation cartridge and evaporated in vacuo. The crude material was dissolved in MeCN/DMSO 1:1 and purified by MDAP. The desired fractions were collected and concentrated under vacuo giving the title compound (103 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08536183B2
出典データセットuspto-grants-2013_09
ORD IDord-c38249caf2674a54ad692beb27cfd819
出典メモuspto-grants-2013_09