تفاعل #969872

معادلة التفاعل

Boc-Val-Pro-OH

1-hydroxibenzotriazol

N,N-diisopropylcarbodiimide

Ara-C

→

Ara-C-dipeptide

المردود 21.0%

Boc-Val-Pro Ara-C

المردود 21.0%

المذيبات

dimethylformamide

ظروف التفاعل

المعالجة

1. 1
   أخرىThen, the solvent was evaporated
2. 2
   workup.DISSOLUTIONthe residue was dissolved in ethyl acetate
3. 3
   غسيلwashed with citric acid (10%), NaHCO3 (10%) and brine
4. 4
   تجفيفThe organic layer was dried (Na2SO4)
5. 5
   أخرىevaporated
6. 6
   أخرىto give a residue that
7. 7
   أخرىwas purified by CCTLC on the chromatotron with dichloromethane:methanol (20:1)

الإجراء التجريبي

A solution of Boc-Val-Pro-OH (94.5 mg, 0.30 mmol) in dimethylformamide (1.5 mL), was successively treated, at room temperature, with 1-hydroxibenzotriazol (40.5 mg, 0.30 mmol), N,N-diisopropylcarbodiimide (46.7 μL, 0.30 mmol) and Ara-C (60.9 mg, 0.25 mmol). The stirring was continued until complete disappearance of the starting material (overnight stirring). Then, the solvent was evaporated, the residue was dissolved in ethyl acetate and washed with citric acid (10%), NaHCO3 (10%) and brine. The organic layer was dried (Na2SO4) and evaporated to give a residue that was purified by CCTLC on the chromatotron with dichloromethane:methanol (20:1) to yield Ara-C-dipeptide (A) (21% yield)

المصدر