تفاعل #11751

معادلة التفاعل

(5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetic acid

sulfamide

→

title compound

المردود 12.7%

N-[(5-Chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetyl]-sulfamide

المردود 12.7%

المذيبات

thionyl chloride

ظروف التفاعل

المعالجة

1. 1
   تركيزThe reaction was concentrated to dryness
2. 2
   workup.DISSOLUTIONthe crude acid chloride was dissolved in 1,4-dioxane (4 mL)
3. 3
   تركيزThe reaction was concentrated
4. 4
   أخرىchromatographed on silica gel

الإجراء التجريبي

A solution of (5-chloro-2-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-phenyl)-acetic acid (0.10 g, 0.21 mmol) in thionyl chloride (2 mL) was stirred at ambient temperature for two hours. The reaction was concentrated to dryness and the crude acid chloride was dissolved in 1,4-dioxane (4 mL) followed by addition of sulfamide (0.022 g, 0.23 mmol). The reaction was stirred at ambient temperature for 3 days. The reaction was concentrated and chromatographed on silica gel to give the title compound (0.014 g, LRMS: 525.1).

المصدر