تفاعل #599748

معادلة التفاعل

2-{2-methoxy-5-[(E)-3-oxo-3-(3,4,5-trimethoxy phenyl)-1-propenyl]phenoxy}acetic acid

4-methyl-2-aminobenzothiazole

1-Ethyl-3-(3-Dimethylaminopropyl)carbodiimide

1-hydroxy-1,2,3-benzotriazole

→

product ( 9k )

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

المذيبات

water

dichloromethane

ظروف التفاعل

المعالجة

1. 1
   استخلاصextracted with dichloromethane
2. 2
   أخرىThe solvent was evaporated under vacuum
3. 3
   أخرىto afford the crude product
4. 4
   أخرىThis was further purified by column chromatography

الإجراء التجريبي

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)

المصدر