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HRID 1947638作成日:2026年10月23日

Pyridine → 1-methyl-1H-pyrazole-3-sulfonic acid benzyl-(1-oxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-amide

https://huagongshe.com/ja/reaction/1947638

反応式

関与物質

役割名称HCID仕込み量
反応物PyridineHCID 1049—
反応物1-Methyl-1H-pyrazole-3-sulfonyl chlorideHCID 13474466—
反応物6-benzylamino-3,4-dihydro-2H-isoquinolin-1-oneHCID 67223915—
溶媒AcetonitrileHCID 6342—
生成物1-methyl-1H-pyrazole-3-sulfonic acid benzyl-(1-oxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-amideHCID 6722399814%

反応条件

温度150 °C

反応手順

To a stirred solution of 6-benzylamino-3,4-dihydro-2H-isoquinolin-1-one (45 mg, 0.18 mmol) and pyridine (31 μl, 0.39 mmol) in anhydrous acetonitrile (1 ml) was added 1-methyl-1H-pyrazole-3-sulfonyl chloride (70 mg, 0.39 mmol) and the reaction heated to 150° C. in a microwave for 0.5 hrs. The solvent was evaporated in vacuo and the crude residue purified by preparative tlc (5% methanol in dichloromethane) to afford the title compound as a yellow solid (10 mg, 14%). HPLC retention time 3.83 min. Mass spectrum (ES+) m/z 397 (M+H).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08399481B2
出典データセットuspto-grants-2013_03
ORD IDord-c56c91d3a32c4bb49b4d22546a0e637f
出典メモuspto-grants-2013_03