تفاعل #2391632

معادلة التفاعل

Boc-Gly-Phe-Leu-OH

N-hydroxysuccinimide

H-Gly-OBzl

N,N′-dicyclohexylcarbodiimide

→

title compound

المردود 62.3%

Boc-Gly-Phe-Leu-Gly-OBzl

المردود 62.3%

المذيبات

N,N-dimethylformamide

tosylate

N,N-dimethylformamide

triethylamine

ظروف التفاعل

المعالجة

1. 1
   workup.ADDITIONwas added
2. 2
   أخرىto react
3. 3
   workup.STIRRINGwith stirring at room temperature for 16 hours
4. 4
   أخرىThis reaction mixture was evaporated to dryness under reduced pressure
5. 5
   أخرىthe residue was purified by silica gel column chromatography (eluent: dichloromethane:methanol=50:1 solution)

الإجراء التجريبي

The Boc-Gly-Phe-Leu-OH obtained in Example 18 (2.4 g) and N-hydroxysuccinimide (656 mg) were dissolved in N,N-dimethylformamide (50 ml), cooled to 4° C., and then added with N,N′-dicyclohexylcarbodiimide (1.17 g) and stirred for 2 hours. To this solution, a N,N-dimethylformamide solution (40 ml), in which tosylate of H-Gly-OBzl (1.9 g) and triethylamine (0.79 ml) had been dissolved, was added and the mixture was allowed to react with stirring at room temperature for 16 hours. This reaction mixture was evaporated to dryness under reduced pressure, and the residue was purified by silica gel column chromatography (eluent: dichloromethane:methanol=50:1 solution) to give the title compound (2.0 g).

المصدر