HRID1108548

反应详情

EQUATION

反应方程式

HRID 1108548 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

2

CONDITIONS

反应条件

温度
0 °C

PROCEDURE

实验过程

A 100 mg portion of Boc-(D)-Arg(Cbz2)-Gly-Arg(Tos)-Thiazole, 1 mL of anisole and 4 drops of MeSEt were placed in HF-cleavage vessel and cooled under liquid N2. HF (10 mL) was then condensed into the reaction mixture and stirred at 0° C. for 1.25 h. HF was removed under vacuum to give a gum-like residue which was titrated with 20 mL of 50% Et2O-hexane and the organic wash removed by filtration. The gum residue was dissolved in 30 mL of 30% aq. HOAc and filtered through the above sintered funnel. The filtrate was lyophilized to give a powder which was purified by RP-HPLC to give 28 mg (60% yield) of (D)-Arg-Gly-Arg-thiazole. FAB-MS (M+H)+ =455.2

WORKUP

后处理

  1. customcondensed into the reaction mixture
  2. customHF was removed under vacuum
  3. customto give a gum-like residue which
  4. washthe organic wash
  5. customremoved by filtration
  6. dissolutionThe gum residue was dissolved in 30 mL of 30% aq. HOAc
  7. filtrationfiltered through the above sintered funnel
  8. customto give a powder which
  9. customwas purified by RP-HPLC