تفاعل #46164

معادلة التفاعل

diisopropyl azodicarboxylate

hydroxyethylmorpholine

triphenyl phosphine

6-Hydroxy-1-oxo-3-phenyl-1H-indene-2-carboxylate isopropyl amide

→

6-(2-morpholine-4-yl ethoxy)-1-oxo-3-phenyl-1H-indene-2-carboxylate isopropyl amide

المردود 99.0%

المذيبات

benzene

tetrahydrofuran

ظروف التفاعل

المعالجة

1. 1
   أخرىwas adjusted to 0° C.
2. 2
   غسيلThe mixture was washed with brine
3. 3
   استخلاصextracted with ethyl acetate
4. 4
   تجفيفThe separated organic layer was dried over anhydrous magnesium sulfate
5. 5
   تركيزconcentrated
6. 6
   أخرىthe resulting residue was purified by column chromatography

الإجراء التجريبي

6-Hydroxy-1-oxo-3-phenyl-1H-indene-2-carboxylate isopropyl amide (7.0 g, 22.78 mmol) was dissolved in tetrahydrofuran:benzene (150 ml:50 ml). Then, hydroxyethylmorpholine (3.59 g, 27.33 mmol) and triphenyl phosphine (7.17 g, 27.33 mmol) were added thereto. When the temperature was adjusted to 0° C., diisopropyl azodicarboxylate (5.53 g, 27.33 mmol) was added dropwise to the mixture followed by stirring for 2 hours at room temperature. The mixture was washed with brine and extracted with ethyl acetate. The separated organic layer was dried over anhydrous magnesium sulfate, concentrated, and the resulting residue was purified by column chromatography to obtain 6-(2-morpholine-4-yl ethoxy)-1-oxo-3-phenyl-1H-indene-2-carboxylate isopropyl amide (9.5 g, yield 99%).

المصدر