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HRID 417883作成日:2026年10月24日

Methanol → 5-(but-3-en-1-ynyl)-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-2-amine

https://huagongshe.com/ja/reaction/417883

反応式

関与物質

役割名称HCID仕込み量
反応物MethanolHCID 887—
反応物Cesium fluorideHCID 25953—
反応物4-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-5-yl)but-3-ynyl 4-methylbenzenesulfonateHCID 86608232—
溶媒DimethylformamideHCID 6228—
溶媒DichloromethaneHCID 6344—
生成物5-(but-3-en-1-ynyl)-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-2-amineHCID 5771381379.7%

反応条件

温度70 °C

反応手順

A mixture of 4-(2-amino-4-chloro-7-((4-methoxy-3,5-dimethylpyridin-2-yl)methyl)-7H-pyrrolo [2,3-d]pyrimidin-5-yl)but-3-ynyl 4-methylbenzenesulfonate (516 mg) and CsF (2.0 g) in DMF (7.0 mL) was heated to 70° C. for 1 h. Work-up and flash chromatography (1→3% MeOH in DCM) gave the title compound (280 mg), as a pale yellow oil. HPLC Rt=5.90 min.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08093229B2
出典データセットuspto-grants-2012_01
ORD IDord-cb43ebc047014c71ba633469e0cfbeb8
出典メモuspto-grants-2012_01