反应 #2446077

反应方程式

BOC-L-alanine

diisopropylcarbodiimide

auristatin F hydroxypropylamide

Auristatin F hydroxypropylamide

→

title compound

收率 75.0%

Auristatin F hydroxypropylamide Boc-L-Alanine

收率 75.0%

溶剂

dichloromethane

反应条件

后处理

1. 1
   workup.ADDITIONwas added
2. 2
   温度The reaction mixture was warmed to 23° C.
3. 3
   其他Purification via preparative HPLC
4. 4
   其他followed by removal of the water via lyophilization

实验过程

BOC-L-alanine (117.0 mg, 0.618 mmol) and DMAP (94.0 mg, 0.772 mmol) were taken up in dichloromethane and then diisopropylcarbodiimide (52.6 μL, 0.340 mmol) was added. The reaction mixture was cooled to 0° C. and stirred for 10 minutes after which auristatin F-hydroxypropylamide (124 mg, 0.154 mmol, prepared as described in Example 48) was added. The reaction mixture was warmed to 23° C. and stirred for 18 hours. Purification via preparative HPLC followed by removal of the water via lyophilization afforded the title compound as beige solid (112 mg, 75% yield).

来源