反応 #10466

反応方程式

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

EDCI

triethylamine

morpholine

→

desired product

収率 10.0%

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

収率 10.0%

溶媒

CH2Cl2

DMF

反応条件

後処理

1. 1
   洗浄The reaction mixture was then washed with 1 M HCl (2×15 mL)
2. 2
   その他the organic layer was collected
3. 3
   乾燥The organic phase was dried (MgSO4)
4. 4
   濃縮concentrated under reduced pressure
5. 5
   その他Purification

実験手順

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.

出典