反应详情

To a solution of HATU (0.253 g) in DMF (3 ml) was added 1-(1-methylethyl)-1H-pyrazole-5-carboxylic acid (0.102 g) and DIPEA (0.211 ml) and the mixture was left to stand for 10 min. 6-(1H-Indol-4-yl)-1H-indazol-4-amine (0.075 g) dissolved in DMF (3 ml) was added and the solution was left to stand at RT for 18 h. DMF was removed by blow down (not to dryness) and the residue was dissolved in chloroform (1 ml) and loaded onto an aminopropyl SPE (2 g) (pre-conditioned with methanol (6 ml) and chloroform (6 ml)). The mixture was left on the column for 2 h then eluted with ethyl acetate:methanol (1:1, 10 ml). The solvent was blown down to dryness and the residue was dissolved in DMSO:methanol (1 ml, 1:1) and purified by MDAP (method K). The solvent was removed in vacuo and dried in an vacuum oven (50° C.) overnight to give title compound, 18 mg.

1. waitthe mixture was left
2. additionwas added
3. waitthe solution was left
4. waitto stand at RT for 18 h
5. customDMF was removed by blow down (not to dryness) and the residue
6. dissolutionwas dissolved in chloroform (1 ml)
7. waitThe mixture was left on the column for 2 h
8. washthen eluted with ethyl acetate:methanol (1:1, 10 ml)
9. dissolutionthe residue was dissolved in DMSO
10. custommethanol (1 ml, 1:1) and purified by MDAP (method K)
11. customThe solvent was removed in vacuo
12. customdried in an vacuum oven (50° C.) overnight