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HRID 1876546作成日:2026年10月27日

2,5-Dimethylpiperazine, trans- → 5-[8-(trans-2,5-Dimethylpiperazin-1-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-2-yl]pyrimidin-2-amine

https://huagongshe.com/reaction/1876546

反応式

関与物質

役割名称HCID仕込み量
反応物2,5-Dimethylpiperazine, trans-HCID 220672—
反応物5-(8-Chloro-9-isobutyl-6-morpholino-9H-purin-2-yl)pyrimidin-2-amineHCID 59333549—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物5-[8-(trans-2,5-Dimethylpiperazin-1-yl)-9-isobutyl-6-morpholin-4-yl-9H-purin-2-yl]pyrimidin-2-amineHCID 6665871298.9%

反応条件

温度150 °C

反応手順

trans-2,5-Dimethylpiperazine (150 mg, 1.3 mmol) and N-methylpyrrolidone (1 ml) were added to 5-(8-chloro-9-isobutyl-6-morpholin-4-yl-9H-purin-2-yl)pyrimidin-2-amine (100 mg, 0.26 mmol) and the resulting mixture was stirred at 150° C. for 48 hours. The reaction mixture was cooled and partitioned with methylene chloride and water, the organic layer was dried over magnesium sulfate, and the solvent was concentrated under reduced pressure. The residue was purified by preparative HPLC (column, NOMURA Develosil Combi-RP-5; mobile phase, acetonitrile/water/formic acid) to give the title compound (120 mg) as a pale yellow solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08309546B2
出典データセットuspto-grants-2012_11
ORD IDord-85eb8076f55e404abe880280f47a8e3d
出典メモuspto-grants-2012_11