反応 #623315

反応方程式

3-Acetoxy-4-oxo-10-(2-piperazin-1-yl-ethyl)-4,10-dihydro-benzo[4,5]imidazo[1,2-α]pyrimidine-2-carboxylic acid methyl ester

diisopropylethylamine

methoxymethyl chloride

→

desired product

収率 28.0%

3-Acetoxy-10-[2-(4-methoxymethyl-piperazin-1-yl)-ethyl]-4-oxo-4,10-dihydro-benzo[4,5]imidazo[1,2-α]pyrimidine-2-carboxylic acid methyl ester

収率 28.0%

溶媒

Dichloromethane

反応条件

後処理

1. 1
   その他were evaporated
2. 2
   その他the residue purified by column chromatography (98:1.5:0.5 dichloromethane: methanol: aqueous ammonia)

実験手順

3-Acetoxy-4-oxo-10-(2-piperazin-1-yl-ethyl)-4,10-dihydro-benzo[4,5]imidazo[1,2-α]pyrimidine-2-carboxylic acid methyl ester (Example 15.3) (97 mg, 0.235 mmol) was dissolved in Dichloromethane (1 mL) and to it was added diisopropylethylamine (95 μL, 0.52 mmol), followed by methoxymethyl chloride (20 μA, 0.258 mmol). The reaction was stirred at room temperature for 24 h before the solvents were evaporated and the residue purified by column chromatography (98:1.5:0.5 dichloromethane: methanol: aqueous ammonia) to afford the desired product (30 mg, 28%).

出典