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HRID 718260作成日:2026年10月25日

Diisopropylethylamine → 5-Amino-2-[2-(4-fluorophenyl)ethyl]-7-(4-benzoylpiperidine-1-yl)-thiazolo[5,4-d]pyrimidine

https://huagongshe.com/reaction/718260

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物4-Benzoylpiperidine hydrochlorideHCID 2724437—
反応物2-(4-Fluorophenethyl)-7-(methylsulfonyl)thiazolo[5,4-d]pyrimidin-5-amineHCID 50941867—
溶媒AcetonitrileHCID 6342—
生成物5-Amino-2-[2-(4-fluorophenyl)ethyl]-7-(4-benzoylpiperidine-1-yl)-thiazolo[5,4-d]pyrimidineHCID 4691685091.3%

反応手順

To a solution of 5-amino-2-[2-(4-fluorophenyl)ethyl]-7-methanesulfonyl-thiazolo[5,4-d]pyrimidine (50 mg, 0.14 mmol) in acetonitrile (5 ml) was added diisopropylethylamine (0.45 mmol, 74 μL) and 4-benzoylpiperidine hydrogen chloride (0.15 mmol). The reaction mixture was stirred at room temperature for 16 hours whereupon the solvent was removed in vacuo. The resulting residue was purified by flash chromatography on silica, the mobile phase being a mixture of methanol and dichloromethane (in a ratio gradually ranging from 100% CH2Cl2 to 1% CH3OH in CH2Cl2), yielding the pure title compound (59 mg) which was characterized by its mass spectrum: MS m/z (%): 462 ([M+H]+, 100).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09193741B2
出典データセットuspto-grants-2015_11
ORD IDord-cd76e01097b246b2a164731608eed89c
出典メモuspto-grants-2015_11