Reacción #1095853

ord-fbf0beacaa5343119ae2f1e5acb0ca06

Ecuación de reacción

CC#CCOc1ncnc(Cl)c1F
4-(2-butynyloxy)-6-chloro-5-fluoropyrimidine
C1CCNCC1
piperidine
CC#CCOc1ncnc(N2CCCCC2)c1F
4-(2-butynyloxy)-5-fluoro-6-piperidinopyrimidine
Rendimiento 99.2%

Disolventes

Condiciones de reacción

Condiciones detalladas
See reaction.notes.procedure_details.

Tratamiento posterior

  1. 1
    workup.ADDITIONwas added
  2. 2
    Temperaturaunder reflux condition
  3. 3
    Concentraciónconcentrated

Procedimiento

Into 3 ml of ethanol was resolved 0.3 g of 4-(2-butynyloxy)-6-chloro-5-fluoropyrimidine, 0.38 g of piperidine was added therein, and the mixture was stirred for 7 hours under reflux condition. The reaction mixture was cooled to near room temperature and concentrated. The residue was subjected to silica gel column chromatography to obtain 0.37 g of 4-(2-butynyloxy)-5-fluoro-6-piperidinopyrimidine (hereinafter, referred to as Compound (2)).

Fuente

DOI: 10.6084/m9.figshare.5104873.v1Patente: US07973028B2uspto-grants-2011_07