Reacción #2150630

Ecuación de reacción

NaHCO3

Cbz-(L)Glu(OtBu)-OH

HOBT hydrate

EDCI hydrochloride

DIPEA

→

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

Disolventes

DCM

DCM THF

Condiciones de reacción

Tratamiento posterior

1. 1
   Otrothe phases were separated
2. 2
   Lavadophase was washed with a 1M NaHSO4 solution
3. 3
   Secadodried (Na2SO4)
4. 4
   Otroevaporated off

Procedimiento

Cbz-(L)Glu(OtBu)-OH (10 g), HOBT hydrate (5 g), EDCI hydrochloride (6.3 g), intermediate 1.4 (6 g) and DIPEA (10 mL) were dissolved in DCM/THF (1/1, 84 mL). The mixture was stirred at RT for 1 h. DCM and an aq. NaHCO3 solution were added to the mixture and the phases were separated. The org. phase was washed with a 1M NaHSO4 solution, dried (Na2SO4) and evaporated off. CC of the crude (EA/Hept 1/2) offered 13.8 g of the desired compound.

Fuente