反応 #338873

反応方程式

4-((5-fluoro-2-oxoindolin-3-ylidene)methyl)benzoic acid

1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride

hydroxybenzo-triazole

triethylamine

6-aminocaproic acid methyl ester hydrochloride

→

title compound

収率 88.2%

6-(4-((5-fluoro-2-oxoindolin-3-ylidene)methyl)benzamido)-hexanoic acid methyl ester

収率 88.2%

溶媒

brine

DMF

反応条件

後処理

1. 1
   workup.ADDITIONwere added
2. 2
   ろ過The solids were collected by vacuum filtration
3. 3
   洗浄washed with water
4. 4
   その他dried under vacuum

実験手順

4-((5-fluoro-2-oxoindolin-3-ylidene)methyl)benzoic acid (283 mg, 1 mmol) and 8 ml of DMF were stirred at room temperature while 1-Ethyl-3-(3-dimethylaminopropyl)-carbodiimide hydrochloride (394 mg, 2 mmol), hydroxybenzo-triazole (162 mg, 1.2 mmol), triethylamine (404 mg, 4 mmol) and 6-aminocaproic acid methyl ester hydrochloride (219 mg, 1.2 mmol) were added. The mixture was stirred for 24 hours at room temperature. The mixture was diluted with 400 mL of brine. The solids were collected by vacuum filtration, washed with water and dried under vacuum to give the title compound (362 mg, 88% yield) as a brown solid. LC-MS (m/z) 411 (M+1).

出典