反应详情

N-[6-(5-Amino-6-chloro-3-pyridinyl)-2-(tetrahydro-2H-pyran-2-yl)-2H-indazol-4-yl]-2-methyl-1,3-thiazole-4-carboxamide (40 mg) was dissolved in pyridine (1 ml) and cyclopropanesulfonyl chloride (24 mg) was added. The reaction was stirred at RT for 1 h. DMAP (3 mg) and cyclopropanesulfonyl chloride (24 mg) were added and the reaction was stirred for 1 h. Further cyclopropanesulfonyl chloride (48 mg) was added and the reaction stirred overnight. Further cyclopropanesulfonyl chloride (48 mg) was added and the reaction was stirred for 2 h. 2M HCl (aq) and DCM were added and the DCM was separated, passed through a hydrophobic frit and evaporated to dryness. The residue was dissolved in DMSO:methanol (1 ml, 7:3, v/v) and purified by MDAP (method E). The product fraction was evaporated to dryness and methanol (3 ml) and a few drops of 2M HCl (aq) were added and the reaction stirred for 2 h. The reaction was evaporated to dryness to give title compound (12 mg).

1. stirringthe reaction was stirred for 1 h
2. stirringthe reaction stirred overnight
3. stirringthe reaction was stirred for 2 h
4. customthe DCM was separated
5. customevaporated to dryness
6. dissolutionThe residue was dissolved in DMSO
7. custommethanol (1 ml, 7:3, v/v) and purified by MDAP (method E)
8. customThe product fraction was evaporated to dryness and methanol (3 ml) and a few drops of 2M HCl (aq)
9. additionwere added
10. stirringthe reaction stirred for 2 h
11. customThe reaction was evaporated to dryness