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HRID 421394作成日:2026年10月27日

Dicyclohexylcarbodiimide → (2S)-4-{(2S)-4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]-2-methylpiperazin-1-yl}-4-oxobutan-2-ol

https://huagongshe.com/reaction/421394

反応式

関与物質

役割名称HCID仕込み量
反応物DicyclohexylcarbodiimideHCID 10868—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物(S)-3-hydroxybutyric acidHCID 94318—
反応物5-{9-Isobutyl-8-[(3S)-3-methylpiperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amineHCID 59333517—
溶媒DimethylformamideHCID 6228—
生成物(2S)-4-{(2S)-4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]-2-methylpiperazin-1-yl}-4-oxobutan-2-olHCID 5933364048.6%

反応条件

温度40 °C

反応手順

5-{9-Isobutyl-8-[(3S)-3-methylpiperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amine (230 mg, 0.5 mmol), dicyclohexylcarbodiimide (160 mg, 0.77 mmol), 1-hydroxybenzotriazole (70 mg, 0.51 mmol), and (S)-3-hydroxybutyric acid (107 mg, 1.0 mmol) were dissolved in dimethylformamide (5 ml) and the resulting mixture was stirred at 40° C. for 16 hours. The solvent was evaporated under reduced pressure and then the residue was purified by preparative HPLC (column, NOMURA Develosil Combi-RP-5; mobile phase, acetonitrile/water/formic acid) to give the title compound (131 mg, 48%) as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08097622B2
出典データセットuspto-grants-2012_01
ORD IDord-73a7db23add84162b8c07c936ccd22d3
出典メモuspto-grants-2012_01