反应 #969872

反应方程式

Boc-Val-Pro-OH

1-hydroxibenzotriazol

N,N-diisopropylcarbodiimide

Ara-C

→

Ara-C-dipeptide

收率 21.0%

Boc-Val-Pro Ara-C

收率 21.0%

溶剂

dimethylformamide

反应条件

后处理

1. 1
   其他Then, the solvent was evaporated
2. 2
   workup.DISSOLUTIONthe residue was dissolved in ethyl acetate
3. 3
   洗涤washed with citric acid (10%), NaHCO3 (10%) and brine
4. 4
   干燥The organic layer was dried (Na2SO4)
5. 5
   其他evaporated
6. 6
   其他to give a residue that
7. 7
   其他was purified by CCTLC on the chromatotron with dichloromethane:methanol (20:1)

实验过程

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)

来源