تفاعل #10466

معادلة التفاعل

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

EDCI

triethylamine

morpholine

→

desired product

المردود 10.0%

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

المردود 10.0%

المذيبات

CH2Cl2

DMF

ظروف التفاعل

المعالجة

1. 1
   غسيلThe reaction mixture was then washed with 1 M HCl (2×15 mL)
2. 2
   أخرىthe organic layer was collected
3. 3
   تجفيفThe organic phase was dried (MgSO4)
4. 4
   تركيزconcentrated under reduced pressure
5. 5
   أخرىPurification

الإجراء التجريبي

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.

المصدر