反应 #1519146

反应方程式

compound

trans-1-{2-[(3,5-dibromobenzyl)oxy]-2,3-dihydro-1H-inden-1-yl}piperazine dihydrochloride

diisopropylethylamine

5-(chloromethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one

→

expected product

trans-5-[(4-{2-[(3,5-Dibromobenzyl)oxy]-2,3-dihydro-1H-inden-1-yl}piperazin-1-yl)methyl]-2,4-dihydro-3H-1,2,4-triazol-3-one

溶剂

dimethylformamide

dichloromethane

反应条件

后处理

1. 1
   其他prepared
2. 2
   其他evaporated to dryness
3. 3
   其他The residue obtained
4. 4
   洗涤washed
5. 5
   其他dried
6. 6
   过滤filtered
7. 7
   其他evaporated
8. 8
   其他The oil obtained
9. 9
   其他is purified by flash chromatography on silica

实验过程

After reconversion to the base, the compound obtained in Step C of Example 1 (2.14 mmol) is dissolved in 30 ml of dimethylformamide. There are added 0.75 ml (4.28 mmol) of diisopropylethylamine and 314 mg (2.35 mmol) of 5-(chloromethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one prepared according to the method described in Tetrahedron Letters, 2000, 41, 8661. The mixture is stirred for 12 hours at ambient temperature and then evaporated to dryness. The residue obtained is taken up in dichloromethane, washed, dried, filtered and evaporated. The oil obtained is purified by flash chromatography on silica to yield the expected product.

来源