反应 #1031

反应方程式

DMF

cis-N-(3-methoxy-4-piperidinyl)-4-amino-5-chloro-2-((S)-1-methyl-2-butynyl)oxybenzamide

3-(4-fluorophenoxy)propyl bromide

triethylamine

→

title compound

收率 91.8%

cis-N-[1-[3-(4-Fluorophenoxyl)propyl]-3-methoxy-4-piperidinyl]-4-amino-5-chloro-2-((S)-1-methyl-2-butynyl)oxybenzamide

收率 91.8%

溶剂

Ethyl acetate

反应条件

后处理

1. 1
   温度cooled
2. 2
   洗涤The obtained mixture was washed with water thrice
3. 3
   干燥dried over magnesium sulfate
4. 4
   其他The residue was purified by silica gel column chromatography (5% methanol/dichloromethane)

实验过程

A mixture comprising 0.10 g of the cis-N-(3-methoxy-4-piperidinyl)-4-amino-5-chloro-2-((S)-1-methyl-2-butynyl)oxybenzamide, 0.07 g of 3-(4-fluorophenoxy)propyl bromide, 0.20 g of triethylamine and 10 ml of DMF was stirred at 50° C. for 2 hours and cooled. Ethyl acetate was poured into the resulting mixture. The obtained mixture was washed with water thrice, dried over magnesium sulfate, and freed from the solvent. The residue was purified by silica gel column chromatography (5% methanol/dichloromethane) to give 0.13 g of the title compound.

来源