反应 #2487504

ord-f4cf5f0aa3c94afaa63dcefd9380ffc4

反应方程式

N#N
N2
Cn1cncc1C#Cc1ccn2c(-c3cccc(NC(=O)NCC(F)(F)F)c3)cnc2c1
1-{3-[7-(3-methyl-3H-imidazol-4-ylethynyl)-imidazo[1,2-a]pyridin-3-yl]-phenyl}-3-(2,2,2-trifluoro-ethyl)-urea
Cn1cncc1CCc1ccn2c(-c3cccc(NC(=O)NCC(F)(F)F)c3)cnc2c1
product
收率 9.2%
Cn1cncc1CCc1ccn2c(-c3cccc(NC(=O)NCC(F)(F)F)c3)cnc2c1
1-(3-{7-[2-(3-Methyl-3H-imidazol-4-yl)-ethyl]-imidazol[1,2-a]pyridin-3-yl}-phenyl)-3-(2,2,2-trifluoro-ethyl)-urea
收率 9.2%

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    workup.ADDITIONThe flask was filled with H2
  2. 2
    过滤The reaction was filtered
  3. 3
    浓缩the filtrate concentrated in vacuo
  4. 4
    其他The crude product was purified by preparative HPLC

实验过程

To an evacuated flask back-filled with N2 containing 1-{3-[7-(3-methyl-3H-imidazol-4-ylethynyl)-imidazo[1,2-a]pyridin-3-yl]-phenyl}-3-(2,2,2-trifluoro-ethyl)-urea (65.7 mg, 0.15 mmol) in MeOH was added Pd (10 wt % on activated carbon) (25.5 mg). The flask was filled with H2 and the reaction stirred for a total of 7.5 hours. The reaction was filtered and the filtrate concentrated in vacuo. The crude product was purified by preparative HPLC to give pure product (6.1 mg). MS: [M+H]+443.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08796244B2uspto-grants-2014_08