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 (50 mg) was dissolved in pyridine (1 ml) and 5-methyl-2-(methyloxy)benzenesulfonyl chloride (35 mg) was added. The reaction was stirred at RT overnight. Further 5-methyl-2-(methyloxy)benzenesulfonyl chloride (35 mg) was added and the reaction was stirred at RT for 4 h. DMAP (3 mg) followed by 5-methyl-2-(methyloxy)benzenesulfonyl chloride (20 mg) was added and the reaction was stirred at RT overnight. The reaction was neutralised with 2M HCl (aq) and extracted into DCM. The DCM was evaporated and the residue was dissolved in DMSO:methanol (1 ml, 8:1, v/v) and purified by MDAP (method E). The desired 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 (39 mg).

1. stirringthe reaction was stirred at RT for 4 h
2. additionwas added
3. stirringthe reaction was stirred at RT overnight
4. extractionextracted into DCM
5. customThe DCM was evaporated
6. dissolutionthe residue was dissolved in DMSO
7. custommethanol (1 ml, 8:1, v/v) and purified by MDAP (method E)
8. customThe desired 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