反応 #1031

反応方程式

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

収率 91.8%

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

収率 91.8%

溶媒

Ethyl acetate

反応条件

後処理

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

実験手順

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.

出典