反应 #1726657

反应方程式

DIPC

camptothecin

N,N-Bis CBZ-Lysine

→

CBZ-Lys

溶剂

methylene chloride

反应条件

后处理

1. 1
   洗涤The solution was washed with 0.1 N HCl
2. 2
   其他dried
3. 3
   其他evaporated under reduced pressure
4. 4
   其他to yield a light yellow solid, which
5. 5
   其他was recrystallized from methanol

实验过程

N,N-Bis CBZ-Lysine (311 mg, 0.75 mmol) was dissolved in 56 mL of anhydrous methylene chloride at room temperature. To this solution were added DIPC (0.12 mL, 0.75 mmol), DMAP (0.61 mg, 0.5 mmol) and camptothecin (0.087 g, 0.25 mmol) at 0° C. The reaction mixture was allowed to warm to room temperature and left for 16 h. The solution was washed with 0.1 N HCl, dried and evaporated under reduced pressure to yield a light yellow solid, which was recrystallized from methanol to give camptothecin-20-ester of N,N-Bis CBZ-Lys 13. Purification of 13 was satisfactory based on TLC and HPLC analysis.

来源