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HRID 16436作成日:2026年10月25日

Hydrochloric Acid → N-[2-Amino-6-(4-pyridinyl)-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)-phenyl]amine

https://huagongshe.com/reaction/16436

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物Sodium BicarbonateHCID 516892—
反応物5-(4-Amino-2-fluorophenoxy)-1H-indazoleHCID 17979271—
反応物4-Chloro-6-(pyridin-4-yl)pyrimidin-2-amineHCID 22324286—
溶媒WaterHCID 962—
生成物N-[2-Amino-6-(4-pyridinyl)-4-pyrimidinyl]-N-[3-fluoro-4-(1H-indazol-5-yloxy)-phenyl]amineHCID 17979346—

反応条件

温度100 °C

反応手順

600 mg (2.47 mmol) of 5-(4-amino-2-fluorophenoxy)-1H-indazole (from example XII) are suspended in 100 ml of water. 510 mg (2.47 mmol) of 4-chloro-6-(4-pyridinyl)-2-pyrimidineamine (from example XXIX) and 0.25 ml of concentrated aqueous hydrogen chloride solution are added, and the mixture is stirred at 100° C. overnight. For work-up, the reaction solution was made alkaline with saturated sodium bicarbonate solution and extracted 3× with ethyl acetate. The precipitate obtained contains crude product and is filtered off with suction. The organic phase is dried with sodium sulfate and concentrated using a rotary evaporator. The residue is combined with the precipitate and 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-6ee620eedb5047d4a28ffc9df009b2cb
出典メモuspto-grants-2010_06