反应详情

4-Methyl-2-morpholinecarboxylic acid hydrochloride (40 mg, 0.22 mmol) was treated with HATU (84 mg, 0.22 mmol) in DMF (0.250 mL) and DIPEA (0.069 mL, 0.40 mmol). The mixture was shaken for five minutes prior to treatment with 6-(1H-indol-4-yl)-1H-indazol-4-amine (25 mg, 0.1 mmol) in DMF (0.25 mL). Reaction mixture was left to stand at room temperature for 18 hrs. Solvent was removed in vacuo and the product re-dissolved in chloroform (0.3 mL) prior to application on to a pre-conditioned (methanol then chloroform) NH2 cartridge (0.5 g). Product was eluted after 2 hr with ethyl acetate/methanol (1:1, 3 mL), and concentrated under a stream of nitrogen using blow down apparatus. Purification by MDAP (Method D) afforded the title compound.

1. customReaction mixture
2. waitwas left
3. waitto stand at room temperature for 18 hrs
4. customSolvent was removed in vacuo
5. dissolutionthe product re-dissolved in chloroform (0.3 mL)
6. washProduct was eluted after 2 hr with ethyl acetate/methanol (1:1, 3 mL)
7. concentrationconcentrated under a stream of nitrogen using blow down apparatus
8. customPurification by MDAP (Method D)