反应 #417991

反应方程式

dichloromethane

3-(3-aminobenzyl)-5-chloro-3H-benzothiazol-2-one

3-(4-methylpiperazin-1-yl)propane 1-chloroformate

DIPEA

→

3-(4-methylpiperazin-1-yl)propyl [3-(5-chloro-2-oxobenzothiazol-3-ylmethyl)phenyl]carbamate

溶剂

THF

反应条件

后处理

1. 1
   洗涤is subsequently washed with 10 ml of 2N NaOH
2. 2
   其他dried
3. 3
   其他evaporated
4. 4
   其他The crude product is purified by means of preparative HPLC

实验过程

173 mg (0.36 mmol) of 3-(3-aminobenzyl)-5-chloro-3H-benzothiazol-2-one and 198 mg (0.67 mmol) of 3-(4-methylpiperazin-1-yl)propane 1-chloroformate are suspended in 3 ml of THF, and 253 μl (1.46 mmol) of DIPEA are added. The reaction mixture is stirred overnight at room temperature. 50 ml of dichloromethane are added to the suspension, which is subsequently washed with 10 ml of 2N NaOH, dried and evaporated. The crude product is purified by means of preparative HPLC. The product “A13” is in the form of the trifluoroacetate.

来源