반응 #10466

반응 방정식

(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)acetic acid

EDCI

triethylamine

morpholine

→

desired product

수율 10.0%

3-chloro-2-methyl-N-[5-(2-morpholin-4-yl-2-oxoethyl)-1,3-thiazol-2yl]benzenesulfonamide

수율 10.0%

용매

CH2Cl2

DMF

반응 조건

후처리

1. 1
   세척The reaction mixture was then washed with 1 M HCl (2×15 mL)
2. 2
   기타the organic layer was collected
3. 3
   건조The organic phase was dried (MgSO4)
4. 4
   농축concentrated under reduced pressure
5. 5
   기타Purification

실험 절차

To a solution of (2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-5-yl)acetic acid (Example 3) (0.09 g, 0.25 mmol) in CH2Cl2 (5.0 mL) and DMF (0.5 mL) were added EDCI (0.05 g, 0.27 mmol), DMAP (0.02 g, 0.12 mmol), triethylamine (0.1 mL, 0.75 mmol) and morpholine (0.03 mL, 0.30 mmol). The reaction mixture was stirred at room temperature overnight. The reaction mixture was then washed with 1 M HCl (2×15 mL) and the organic layer was collected. The organic phase was dried (MgSO4) and concentrated under reduced pressure. Purification using preparative HPLC afforded the desired product (0.01 g) in 10% yield.

출처