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HRID 421297作成日:2026年10月26日

Triethylamine → 5-{9-Isobutyl-8-[4-(methylsulfonyl)piperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amine

https://huagongshe.com/reaction/421297

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Methanesulfonyl chlorideHCID 31297—
反応物5-(9-Isobutyl-6-morpholino-8-(piperazin-1-yl)-9H-purin-2-yl)pyrimidin-2-amineHCID 59333501—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物5-{9-Isobutyl-8-[4-(methylsulfonyl)piperazin-1-yl]-6-morpholin-4-yl-9H-purin-2-yl}pyrimidin-2-amineHCID 4537786151%

反応手順

Triethylamine (143 μl) and mesyl chloride (50 μl, 0.63 mmol) were added to 5-(9-isobutyl-6-morpholin-4-yl-8-piperazin-1-yl-9H-purin-2-yl)pyrimidin-2-amine (2 ml of solution of 100 mg of this compound in 1 ml of NMP) and the resulting mixture was stirred for 1 hour. Mesyl chloride (50 μl, 0.63 mmol) was further added, the resulting mixture was stirred for 1 hour, then the reaction mixture was partitioned with ethyl acetate and water, and the organic layer was dried over magnesium sulfate. The solvent was evaporated under reduced pressure and the residue was purified by preparative HPLC (column, NOMURA Develosil Combi-RP-5; mobile phase, acetonitrile/water/formic acid) to give the title compound (135 mg, 51%) as a pale yellow 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-122a053be12a49d19c490a9d3b62a4fa
出典メモuspto-grants-2012_01