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HRID 512566作成日:2026年10月27日

2-Amino-4-methylbenzothiazole → N1-(4-methyl-1,3-benzothiazol-2-yl)-2-{2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxy phenyl)-1-propenyl]phenoxy}acetamide

https://huagongshe.com/reaction/512566

反応式

関与物質

役割名称HCID仕込み量
反応物2-Amino-4-methylbenzothiazoleHCID 15132—
反応物1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimideHCID 15908—
反応物1-HydroxybenzotriazoleHCID 75771—
反応物2-{2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxy phenyl)-1-propenyl]phenoxy}acetic acidHCID 56968190—
溶媒WaterHCID 962—
溶媒DichloromethaneHCID 6344—
生成物N1-(4-methyl-1,3-benzothiazol-2-yl)-2-{2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxy phenyl)-1-propenyl]phenoxy}acetamideHCID 60151529802%

反応手順

To a solution of 4-methyl-2-aminobenzothiazole (164 mg, 1.0 mmol) in dichloromethane (20 mL) was added 1-Ethyl-3-(3-Dimethylaminopropyl)carbodiimide (EDC) (191 mg, 1.0 mmol) and 1-hydroxy-1,2,3-benzotriazole (HOBt) (13.5 mg, 0.1 mmol). Then added 2-{2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxy phenyl)-1-propenyl]phenoxy}acetic acid (2) (402 mg, 0.1 mmol) and the reaction mixture was stirred at a temperature of 25° C. for 24 h and the reaction was monitored by TLC. Then to this water is added and extracted with dichloromethane. The solvent was evaporated under vacuum to afford the crude product. This was further purified by column chromatography using ethyl acetate and hexane as solvent system to obtain the pure product (9k) (440 mg, 80% yield)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09102638B2
出典データセットuspto-grants-2015_08
ORD IDord-d417c5f001554fca95dba4525fa98a2b
出典メモuspto-grants-2015_08