تفاعل #2286355

معادلة التفاعل

triethylamine

2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1,3-thiazole-4-carboxylic acid

methoxy(methyl)ammonium chloride

1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide HCl salt

→

tert-Butyl 4-{4-[methoxy(methyl)carbamoyl]-1,3-thiazol-2-yl}piperidine-1-carboxylate

المذيبات

dichloromethane

water

ظروف التفاعل

المعالجة

1. 1
   workup.STIRRINGThe mixture was stirred at room temperature overnight
2. 2
   أخرىThe aqueous phase was separated off
3. 3
   استخلاصextracted with ethyl acetate
4. 4
   تجفيفThe combined organic phases are dried over sodium sulphate
5. 5
   تركيزconcentrated under reduced pressure
6. 6
   أخرىThe residue was purified chromatographically

الإجراء التجريبي

At room temperature, triethylamine (324 mg) was added to a suspension of 2-[1-(tert-butoxycarbonyl)piperidin-4-yl]-1,3-thiazole-4-carboxylic acid (1.0 g) in dichloromethane (30 mL). After ten minutes of stirring, methoxy(methyl)ammonium chloride (312 mg), 4-dimethylaminopyridine (39 mg) and 1-ethyl-3-(3′-dimethylaminopropyl)carbodiimide HCl salt (675 mg) were added. The mixture was stirred at room temperature overnight, and water was then added. The aqueous phase was separated off and extracted with ethyl acetate. The combined organic phases are dried over sodium sulphate and concentrated under reduced pressure. The residue was purified chromatographically. This gave tert-butyl 4-{4-[methoxy(methyl)carbamoyl]-1,3-thiazol-2-yl}piperidine-1-carboxylate (1.0 g).

المصدر