HRID1748

反应详情

EQUATION

反应方程式

HRID 1748 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

2

CONDITIONS

反应条件

温度
4 °C

PROCEDURE

实验过程

Fmoc-Gly-Pro-Hyp was synthesized from Gly-Pro-Hyp as follows: 3.0 g Gly-Pro-Hyp (10.5 mmol) was dissolved in 54 mL Na2CO3 --H2O (1:9) and stored at 4° C. 4.05 g 9-fluorenylmethyl succinimidyl carbonate (12.0 mmol) was dissolved in 45 mL dimethoxyethane and stirred at 4° C. The aqueous Na2CO3 solution was added slowly to the dimethoxyethane solution, and the reaction proceeded for 2.5 h at 4° C. and 21 h at room temperature. The solution was filtered, and 360 mL H2O was added to the filtrate. The aqueous layer was extracted with 300 mL of diethyl ether, acidified to pH 2 with concentrated HCl, reduced to half volume at 80° C. under reduced pressure, and stored at 4° C. for 24 h. The aqueous layer was decanted from the oily precipitate, reduced to ~30 mL at 81° C. under reduced pressure, and stored at 4° C. for 24 h. The aqueous layer was decanted from the oily precipitate. Both oily precipitates were dissolved in a total of 20 mL methanol, then 250 mL ethyl acetate was added. A white residue was recovered by evaporation at 73° C. for 1 h under reduced pressure; yield 3.23 g (6.39 mmol, 60.6%). The identity of the product as Fmoc-Gly-Pro-Hyp and its homogeneity was verified by thin layer chromatography [chloroform-methanol-HOAc (95:20:3)], scanning UV spectroscopy, and Edman degradation sequence analysis.

WORKUP

后处理

  1. customstored at 4° C
  2. filtrationThe solution was filtered
  3. addition360 mL H2O was added to the filtrate
  4. extractionThe aqueous layer was extracted with 300 mL of diethyl ether
  5. customreduced to half volume at 80° C. under reduced pressure
  6. waitstored at 4° C. for 24 h
  7. customThe aqueous layer was decanted from the oily precipitate
  8. customreduced to ~30 mL at 81° C. under reduced pressure
  9. waitstored at 4° C. for 24 h
  10. customThe aqueous layer was decanted from the oily precipitate
  11. customBoth oily precipitates
  12. dissolutionwere dissolved in a total of 20 mL methanol
  13. addition250 mL ethyl acetate was added
  14. customA white residue was recovered by evaporation at 73° C. for 1 h under reduced pressure