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HRID 421391作成日:2026年10月27日

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

https://huagongshe.com/reaction/421391

反応式

関与物質

役割名称HCID仕込み量
反応物1-HydroxybenzotriazoleHCID 75771—
反応物(S)-3-hydroxybutyric acidHCID 94318—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
反応物5-(9-Isobutyl-6-morpholino-8-(piperazin-1-yl)-9H-purin-2-yl)pyrimidin-2-amineHCID 59333501—
溶媒DimethylformamideHCID 6228—
生成物(2S)-4-{4-[2-(2-Aminopyrimidin-5-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-8-yl]piperazin-1-yl}-4-oxobutan-2-olHCID 5475475756%

反応手順

5-(9-Isobutyl-6-morpholin-4-yl-8-piperazin-1-yl-9H-purin-2-yl)pyrimidin-2-amine (150 mg, 0.33 mmol), 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride (128 mg, 0.67 mmol), 1-hydroxybenzotriazole (45 mg, 0.33 mmol), and (S)-3-hydroxybutyric acid (70 mg, 0.67 mmol) were dissolved in dimethylformamide (5 ml) and the resulting mixture was stirred 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 (97 mg, 56%) 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-89be7a3eb91f49e680bdc3b8ec25a34e
出典メモuspto-grants-2012_01