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HRID 1958378作成日:2026年10月27日

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

https://huagongshe.com/reaction/1958378

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物1,1'-CarbonyldiimidazoleHCID 68263—
反応物CyclopentanemethanolHCID 77195—
反応物1-(4-methanesulfonyl-phenyl)-4-(piperidin-4-yloxy)-1H-pyrazolo[3,4-d]pyrimidineHCID 11360802—
溶媒Dimethyl SulfoxideHCID 679—
生成物4-[1-(4-Methanesulfonyl-phenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yloxy]-piperidine-1-carboxylic acid cyclopentylmethyl esterHCID 2189780935.3%

反応手順

Di-imidazol-1-yl-methanone (0.51 mmol, 83 mg), and cyclopentyl-methanol (0.51 mmol, 51 mg) were dissolved in DMSO (1 mL) and stirred for 30 minutes at room temperature. Then, 1-(4-methanesulfonyl-phenyl)-4-(piperidin-4-yloxy)-1H-pyrazolo[3,4-d]pyrimidine (0.17 mmol, 70 mg) and triethylamine (0.51 mmol, 72 μL) were added and heated in a microwave at 120° C. for 6 minutes. The progress of the reaction was monitored by LCMS. The reaction mixture was quenched with water and the product was extracted with ethylacetate. Removal of organic solvents in vacuo and purification by HPLC provided Compound A120 as a white solid (30 mg, 29%). Exact mass calculated for C24H29N5O5S 499.58, found 500.4 (MH+).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08410119B2
出典データセットuspto-grants-2013_04
ORD IDord-ee2abcd086a340d1bcebcb06fd6a716d
出典メモuspto-grants-2013_04