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HRID 1958433作成日:2026年10月26日

Sodium hydride → 3-[1-(2-Fluoro-4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-pyrrolidine-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/1958433

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium hydrideHCID 24758—
反応物1-Boc-3-pyrrolidinolHCID 4416939—
反応物4-Chloro-1-(2-fluoro-4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidineHCID 21897661—
溶媒TetrahydrofuranHCID 8028—
生成物3-[1-(2-Fluoro-4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-pyrrolidine-1-carboxylic acid tert-butyl esterHCID 5363041667.8%

反応手順

A mixture of 3-hydroxy-pyrrolidine-1-carboxylic acid tert-butyl ester (431 mg, 2.3 mmol) and sodium hydride (92 mg, 3.82 mmol) in THF (10 mL) was stirred for 30 minutes at room temperature. Then 4-chloro-1-(2-fluoro-4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidine (500 mg, 1.53 mmol) was added and stirred overnight at room temperature. The reaction mixture was quenched with water and the product extracted with ethyl acetate. The ethylacetate layer was dried over MgSO4, concentrated in vacuo, and purified by flash chromatography to afford compound A140 as a white solid (495 mg, 45%). Exact mass calculated for C21H24FN5O5S 477.15, found 478.2 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08410119B2
出典データセットuspto-grants-2013_04
ORD IDord-7d469ada9f3144df87831c0277e8cc34
出典メモuspto-grants-2013_04