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HRID 421379作成日:2026年10月27日

L-Lactic Acid → (2S)-1-{4-[2-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-9-(2,2,2-trifluoroethyl)-9H-purin-8-yl]piperazin-1-yl}-1-oxopropan-2-ol

https://huagongshe.com/reaction/421379

反応式

関与物質

役割名称HCID仕込み量
反応物L-Lactic AcidHCID 107689—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
反応物5-[6-Morpholin-4-yl-8-piperazin-1-yl-9-(2,2,2-trifluoroethyl)-9H-purin-2-yl]pyrimidin-2-amine trifluoroacetateHCID 86641996—
反応物HCID 178526939HCID 178526939—
溶媒DimethylformamideHCID 6228—
溶媒TriethylamineHCID 8471—
生成物(2S)-1-{4-[2-(2-Aminopyrimidin-5-yl)-6-morpholin-4-yl-9-(2,2,2-trifluoroethyl)-9H-purin-8-yl]piperazin-1-yl}-1-oxopropan-2-olHCID 59333520—

反応手順

L-Lactic acid (17 mg, 0.19 mmol), hydroxybenzotriazole hydrate (37 mg, 0.19 mmol), 1-ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride (37 mg, 0.19 mmol), dimethylformamide (3 ml), and triethylamine (100 μl) were added to 5-[6-morpholin-4-yl-8-piperazin-1-yl-9-(2,2,2-trifluoroethyl)-9H-purin-2-yl]pyrimidin-2-amine trifluoroacetate (120 mg, 0.17 mmol) and the resulting mixture was stirred for 5 hours. The reaction mixture was partitioned with ethyl acetate and water, the organic layer was washed with saturated aqueous sodium bicarbonate solution and dried over magnesium sulfate, and then the solvent was evaporated under reduced pressure. The residue was purified by silica gel chromatography (chloroform:methanol=19:1) to give the title compound as a colorless 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-30a61032169e45608c535bd88a2856e3
出典メモuspto-grants-2012_01