반응 #1915664

반응 방정식

3-(N-tert-butoxycarbonylamino)propanesulfonamide

1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride

(E)-3-{8-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl]-2-morpholino-4-oxo-4H-pyrido -[1,2-a]pyrimidin-3-yl}-2-propenoic acid

ethyl acetate

→

title compound

수율 40.7%

N-((E)-3-{8-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl]-2-morpholino-4-oxo-4H-pyrido-[1,2-a]pyrimidin-3-yl}-2-propenoyl)-3-(tert-butoxycarbonylamino)-1-propane-sulfonamide

수율 40.7%

용매

dimethylformamide

hexane

반응 조건

후처리

1. 1
   세척washed with 0.2 M hydrochloric acid
2. 2
   건조dried over sodium sulfate
3. 3
   기타the solvent was evaporated under reduced pressure
4. 4
   기타The residue was purified by silica gel column chromatography

실험 절차

(E)-3-{8-[2-(4-Isopropyl-1,3-thiazol-2-yl)ethyl]-2-morpholino-4-oxo-4H-pyrido -[1,2-a]pyrimidin-3-yl}-2-propenoic acid (53 mg) was dissolved in dimethylformamide (2 ml), added with 3-(N-tert-butoxycarbonylamino)propanesulfonamide (55 mg) and 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (67 mg), and the mixture was stirred at room temperature for 24 hours. The reaction solution was added with ethyl acetate and hexane, washed with 0.2 M hydrochloric acid, and dried over sodium sulfate, and the solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography to obtain the title compound (32 mg) as yellow powder.

출처