反応 #59790

反応方程式

4-(Piperazine-1-sulfonyl)-morpholine hydrochloride

diisopropylethylamine

4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-1-carbonyl chloride

→

[4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazol-1-yl]-[4-(morpholine-4-sulfonyl)-piperazin-1-yl]-methanone

収率 64.0%

溶媒

methylene chloride

methylene chloride

反応条件

後処理

1. 1
   洗浄washed with water
2. 2
   その他The organic layer was evaporated
3. 3
   その他the residue purified by flash chromatography

実験手順

4-(Piperazine-1-sulfonyl)-morpholine hydrochloride (0.042 mmol) was suspended in methylene chloride, and 400 uL of diisopropylethylamine was added. The mixture was added to 4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazole-1-carbonyl chloride (10 mg, 0.019 mmol, example 3), and the reaction mixture was allowed to stand overnight. It was diluted with methylene chloride and washed with water. The organic layer was evaporated, and the residue purified by flash chromatography using ethyl acetate and hexanes to give [4,5-bis-(4-chloro-phenyl)-2-(2-ethoxy-4-trifluoromethyl-phenyl)-4,5-dihydro-imidazol-1-yl]-[4-(morpholine-4-sulfonyl)-piperazin-1-yl]-methanone (9.0 mg). LR-MS: 740.2 [(M+H)+].

出典