Reaktion #1158875

Reaktionsgleichung

1-tert.-butoxycarbonylmethyl-1H-indole-2-carboxylic acid

N-ethylmorpholine

1-isopropyl-piperidin-4-ylamine hydrochloride

→

tert.-Butyl [2-(1-isopropyl-piperidin-4-ylcarbamoyl)-indol-1-yl]-acetate

Lösungsmittel

dichloromethane

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.STIRRINGthe reaction mixture was further stirred for 1 hour
2. 2
   SonstigeAfter removal of the solvent under reduced pressure the residue
3. 3
   Sonstigewas partitioned between 15 ml water and 15 ml dichloromethane
4. 4
   WaschenThe organic layer was washed with additional water
5. 5
   Trocknendried over sodium sulphate
6. 6
   FiltrationAfter filtration the solvent
7. 7
   Sonstigewas removed under reduced pressure
8. 8
   Sonstigea white solid was obtained
9. 9
   SonstigeThe residue was directly subjected to the subsequent reaction without further purification

Vorschrift

To a solution of 0.5 g 1-tert.-butoxycarbonylmethyl-1H-indole-2-carboxylic acid and 0.91 ml N-ethylmorpholine in 3 ml dichloromethane 0.6 g O-[(ethoxycarbonyl)cyanomethylenamino]-N,N,N′,N′-tetramethyluronium tetrafluoroborate were added and the mixture was stirred for 30 min at room temperature. 0.39 g 1-isopropyl-piperidin-4-ylamine hydrochloride were added to the mixture and the reaction mixture was further stirred for 1 hour. After removal of the solvent under reduced pressure the residue was partitioned between 15 ml water and 15 ml dichloromethane. The organic layer was washed with additional water and then dried over sodium sulphate. After filtration the solvent was removed under reduced pressure and a white solid was obtained. The residue was directly subjected to the subsequent reaction without further purification.

Quelle