HRID322548

反应详情

EQUATION

反应方程式

HRID 322548 的结构方程式

AUXILIARIES

试剂、催化剂与溶剂

1

CONDITIONS

反应条件

温度
0 °C

PROCEDURE

实验过程

To a suspension of Boc—Arg(Tos)—OH (2 g, 4.7 mmol) in DMF (20 mL) at 0° C. was added MeNHOMe.HCl (1 g, 10.3 mmol), DIEA (2 mL) and BOP (2.5 g, 5.6 mmol). The solution was stirred at 0° C. for 10 h. DMF was evaporated in vacuo. The oily residue was dissolved in EtOAc (200 mL) and water (20 mL). The organic layer was washed with sat. NaHCO3, water (20 mL), 1 M HCl (10 mL) and sat. NaCl (2×20 mL). The organic layer was dried over MgSO4, filtered and evaporated to give a suspension. The suspension was filtered, washed with cold EtOAc (10 mL) and dried to give Boc—Arg(Tos)—N(Me)OMe (1.5 g, 70% yield). FAB—MS (M+H)+=472

WORKUP

后处理

  1. customDMF was evaporated in vacuo
  2. dissolutionThe oily residue was dissolved in EtOAc (200 mL)
  3. washThe organic layer was washed with sat. NaHCO3, water (20 mL), 1 M HCl (10 mL) and sat. NaCl (2×20 mL)
  4. dry with materialThe organic layer was dried over MgSO4
  5. filtrationfiltered
  6. customevaporated
  7. customto give a suspension
  8. filtrationThe suspension was filtered
  9. washwashed with cold EtOAc (10 mL)
  10. customdried