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HRID 719462作成日:2026年10月26日

Triethylamine → 4-[1-(4-Methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidine-1-carboxylic acid 2,2-dimethyl-propyl ester

https://huagongshe.com/reaction/719462

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物2,2-Dimethylpropyl carbonochloridateHCID 3352185—
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4-[1-(4-Methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidine-1-carboxylic acid 2,2-dimethyl-propyl esterHCID 2189767533.8%

反応手順

1-(4-Methanesulfonyl-phenyl)-4-(piperidin-4-yloxy)-1H-pyrazolo[3,4-d]pyrimidine hydrochloride (0.17 mmol, 70 mg), neopentyl chloroformate (0.25 mmol, 37 μL) and triethylamine (0.51 mmol, 72 μL) were dissolved in DMF (2 mL) and stirred for 60 minutes at room temperature. Progress of the reaction was monitored by TLC and LCMS. The reaction mixture was quenched with water. The product was extracted with ethyl acetate. Removal of organic solvents in vacuo and purification by HPLC provided Compound A124 as a white solid (28 mg, 27%). Exact mass calculated for C23H29N5O5S 487.57, found 488.20 (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-e0be510e98a54e598d8b6de37f65b688
出典メモuspto-grants-2006_11