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HRID 719463作成日:2026年10月26日

Fusaric Acid → (5-Butyl-pyridin-2-yl)-{4-[1-(4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidin-1-yl}-methanone

https://huagongshe.com/reaction/719463

反応式

関与物質

役割名称HCID仕込み量
反応物Fusaric AcidHCID 3442—
反応物Isopropyl chloroformateHCID 7917—
反応物TriethylamineHCID 8471—
反応物1-(4-Methanesulfonyl-phenyl)-4-(piperidin-4-yloxy)-1H-pyrazolo[3,4-d]pyrimidine hydrochlorideHCID 21897774—
溶媒DimethylformamideHCID 6228—
生成物(5-Butyl-pyridin-2-yl)-{4-[1-(4-methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidin-1-yl}-methanoneHCID 2189778514.3%

反応手順

5-Butyl-pyridine-2-carboxylic acid (92 mg, 0.51 mmol) and isopropyl chloroformate (70 μL, 0.51 mmol) were dissolved in DMF and stirred at room temperature for 40 min. 1-(4-Methanesulfonyl-phenyl)-4-(piperidin-4-yloxy)-1H-pyrazolo[3,4-d]pyrimidine hydrochloride (70 mg, 0.17 mmol) and triethylamine (72 μL, 0.51 mmol) were added next and continued to stir for 24 hours. Progress of the reaction was monitored by TLC and LCMS. Removal of organic solvents in vacuo and purification by HPLC afforded Compound A125 as a white solid (13 mg, 13%). Exact mass calculated for C27H30N6O4S 534.63, found 535.20 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07132426B2
出典データセットuspto-grants-2006_11
ORD IDord-9944c216294d426aa0aa521f149a665f
出典メモuspto-grants-2006_11