Reacción #43386

ord-1df2cfb453494b1a936f45aad2419613

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    workup.ADDITIONmixed for 10 mins on a shaker
  2. 2
    workup.ADDITIONagain mixed in
  3. 3
    FiltraciónAfter 16 h at ambient temperature the mixture is filtered through basic aluminium oxide
  4. 4
    Lavadowashed with DMF/methanol=9:1
  5. 5
    OtroThen it is evaporated down i

Procedimiento

200 μl of a 0.05 molar solution of 4-{2-[(5-chloro-thiophene-2-carbonyl)-amino]-2-methyl-propionylamino}-2-methyl-benzoic acid, which additionally contains 0.05 mol/l DIPEA, in DMF are combined with 100 μl of a 0.1-molar solution of TBTU in DMF on a microtitre plate and mixed for 10 mins on a shaker. Then 200 μl of a 0,05-molar solution of (3-hydroxy-prop-1-yl)-piperidine, which additionally contains 0.05 mol/l DIPEA, are pipetted in and again mixed in by shaking. After 16 h at ambient temperature the mixture is filtered through basic aluminium oxide and washed with DMF/methanol=9:1. Then it is evaporated down i. vac.

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US07732466B2uspto-grants-2010_06