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HRID 41268作成日:2026年10月25日

Sodium Hydroxide → 3-[2,6-Dimethoxy-4-(methoxymethyl)phenyl]-6-(methylsulfonyl)pyrazolo[5,1-b][1,3]thiazole

https://huagongshe.com/reaction/41268

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium HydroxideHCID 14798—
反応物L-ProlineHCID 145742—
反応物Sodium methanesulfinateHCID 2733271—
反応物6-Bromo-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]pyrazolo[5,1-b][1,3]thiazoleHCID 58223418—
触媒Copper iodideHCID 83717—
溶媒Dimethyl SulfoxideHCID 679—
溶媒WaterHCID 962—
生成物3-[2,6-Dimethoxy-4-(methoxymethyl)phenyl]-6-(methylsulfonyl)pyrazolo[5,1-b][1,3]thiazoleHCID 5822345689.7%

反応条件

温度140 °C

反応手順

To a dimethyl sulfoxide (28.0 mL) solution of 6-bromo-3-[2,6-dimethoxy-4-(methoxymethyl)phenyl]pyrazolo[5,1-b][1,3]thiazole (1.12 g, 2.92 mmol) were added sodium methanesulphinate (2.38 g, 23.3 mmol), L-proline (268 mg, 2.33 mmol), sodium hydroxide (184 mg, 4.61 mmol), and copper iodide (444 mg, 2.33 mmol) and the mixture was heated at 140° C. for three hours by using Biotage Initiator™ Microwave Synthesizer. After the reaction was completed, water was added, the reaction mixture was extracted with ethyl acetate, the organic layer was dried over magnesium sulfate, and the solvent was distilled off under reduced pressure. To the residue, ethyl acetate was added, and the obtained solid was subjected to suction filtration and dried to obtain the title compound (1.00 g, 2.62 mmol).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08530504B2
出典データセットuspto-grants-2013_09
ORD IDord-b3466e03091f4f59a6c842bb8b7abe9c
出典メモuspto-grants-2013_09