Reacción #1345546

Ecuación de reacción

Z-(L)Glu(OtBu)-OH

EDCI hydrochloride

HOBT hydrate

DIPEA

DCM THF

→

desired compound

4-((S)-2-benzyloxycarbonylamino-4-tert-butoxycarbonyl-butyryl)-piperazine-1-carboxylic acid butyl ester

Disolventes

water

DCM

Condiciones de reacción

Tratamiento posterior

1. 1
   workup.STIRRINGThe mixture was stirred at RT overnight
2. 2
   Otrothe phases were separated
3. 3
   Lavadophase was washed with 2M Na2CO3, with 1M NaHSO4 and with brine
4. 4
   Secadowas dried (Na2SO4)
5. 5
   Otroevaporated off
6. 6
   OtroDrying under HV

Procedimiento

To a solution of Z-(L)Glu(OtBu)-OH (25.2 g) in DCM/THF (240 mL/60 mL) were added EDCI hydrochloride (17.2 g), HOBT hydrate (13.7 g) and DIPEA (28.2 mL). After stirring at RT for 5 min, intermediate 1.2 (20 g) was added. The mixture was stirred at RT overnight. DCM and water were added and the phases were separated. The org. phase was washed with 2M Na2CO3, with 1M NaHSO4 and with brine, was dried (Na2SO4) and evaporated off. Drying under HV gave the desired compound as an orange oil (40 g).

Fuente