反応 #42792

ord-d270f758becd48d19d8ee195ccff863a

反応方程式

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

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    workup.ADDITIONwas added
  2. 2
    温度under reflux condition
  3. 3
    濃縮concentrated

実験手順

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)).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US07732448B2uspto-grants-2010_06