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HRID 16456作成日:2026年10月26日

Dimethylformamide → N4-[3-Fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-6-morpholin-4-yl-pyrimidine-2,4-diamine

https://huagongshe.com/reaction/16456

反応式

関与物質

役割名称HCID仕込み量
反応物DimethylformamideHCID 6228—
反応物MorpholineHCID 8083—
反応物DiisopropylethylamineHCID 81531—
反応物6-Chloro-N4-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]pyrimidine-2,4-diamineHCID 58733241—
溶媒2-EthylhexanolHCID 7720—
生成物N4-[3-Fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)phenyl]-6-morpholin-4-yl-pyrimidine-2,4-diamineHCID 58733326—

反応条件

温度150 °C

反応手順

52 mg (0.14 mmol) of 6-chloro-N4-[3-fluoro-4-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-phenyl]pyrimidine-2,4-diamine (from example 60) are dissolved in 2.5 ml of 2-ethylhexanol. 0.24 ml of N-ethyldiisopropylamine and 36 mg (0.42 mmol) of morpholine are added, and the mixture is heated at 150° C. bath temperature for 20 hours. After cooling, a little DMF is added and the mixture is chromatographed on silica gel 60 (gradient column: mobile phase: DCM:methanol=50:1, then 3:1). This gives an oil which is purified by preparative HPLC.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07737153B2
出典データセットuspto-grants-2010_06
ORD IDord-f27cdbac85644e37bba24b36a57db768
出典メモuspto-grants-2010_06