反应 #81907

ord-3c1ba819d1914d3589c7b7c92e2c4cb5

反应条件

温度
125°CELSIUS
详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    温度The mixture was heated
  2. 2
    过滤the solids were filtered
  3. 3
    洗涤washed with ethyl acetate
  4. 4
    浓缩The filtrate was concentrated under reduced pressure
  5. 5
    其他The residual gum was triturated with 10 mL of water
  6. 6
    过滤the resulting solid was filtered
  7. 7
    洗涤washed well with water
  8. 8
    其他dried
  9. 9
    其他This crude material was chromatographed
  10. 10
    洗涤The column was eluted with 1:1 (v/v) hexane
  11. 11
    其他ethyl acetate, collecting the fractions that
  12. 12
    其他Evaporation of the solvents
  13. 13
    其他gave a solid
  14. 14
    过滤the crystals were filtered

实验过程

Powdered potassium carbonate (0.8 g; 5.8 mmol) was added to a solution of 0.220 g (1.2 mmol) of the aldehyde from Example 18 and 0.235 g (1.26 mmol) (ca. 5% excess) of 2,6-dichlorophenylacetonitrile in 2.0 mL of dimethylformamide. The mixture was heated with stirring at 125° C. for 6 hours. Ethyl acetate (5 mL) was added to the cooled mixture, and the solids were filtered and washed with ethyl acetate. The filtrate was concentrated under reduced pressure. The residual gum was triturated with 10 mL of water, and the resulting solid was filtered, washed well with water, and dried. This crude material was chromatographed by placing a chloroform solution on a silica gel column wet with chloroform. The column was eluted with 1:1 (v/v) hexane:ethyl acetate, collecting the fractions that contain the Rf 0.25 spot on tlc (1:1 hexane:ethyl acetate). Evaporation of the solvents gave a solid. The solid product was dissolved in about 0.5 mL of methylene chloride. Crystals develop. Petroleum ether (ca. 2 mL) was added, and the crystals were filtered to provide 0.168 g (40%) of 6-(2,6-dichlorophenyl)-8-methyl-2-methylsulfanyl-8H-pyrido[2,3-d]pyrimidin-7-ylideneamine, mp 198°-200° C.;

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US05620981uspto-grants-1997_04