反应详情

温度

105 °C

2,3-Diamino-4,5-dichloropyridine (Example 206a) (0.10 g, 0.56 mmol) and 4-[(2-morpholin-4-ylethyl)amino]benzoic acid (prepared in a manner analogous to Example 206c) (0.14 g, 0.56 mmol) were dissolved in POCl3 (5 ml) and heated to 105° C. for 5 h. The excess of POCl3 was evaporated off and the residue was dissolved in EtOAc and aqueous K2CO3. The aqueous phase was extracted three times with EtOAc. The combined organic phases were washed with brine, dried (Na2SO4), evaporated in vacuo and the residue was purified by HPLC-C18, giving the title product (0.006 g, 2%).

1. customThe excess of POCl3 was evaporated off
2. dissolutionthe residue was dissolved in EtOAc
3. extractionThe aqueous phase was extracted three times with EtOAc
4. washThe combined organic phases were washed with brine
5. dry with materialdried (Na2SO4)
6. customevaporated in vacuo
7. customthe residue was purified by HPLC-C18