反应详情

This compound may be prepared using methods as described for Compound 6, step 4 using (5-bromo-[1,2,4]triazolo[1,5-a]pyrazin-8-yl)-(4-morpholin-4-yl-phenyl)-carbamic acid tert-butyl ester (170 mg, 0.36 mmol), 1,1-dioxo-6-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-1,2-dihydro-1λ6-benzo[d]isothiazol-3-one (374 mg, 0.72 mmol) and Pd(PPh3)4 (100 mg, 0.082 mmol) in 1.5M Na2CO3 (2 mL, 3 mmol) and dioxane (6 mL). Purification of the reaction mixture by silica gel column chromatography using 1:1 petroleum ether:ethyl acetate affords a compound still impure. A second silica gel column chromatography eluting with 10:1 DCM:MeOH affords the title compound (91 mg, 44%).

1. customThis compound may be prepared
2. customPurification of the reaction mixture by silica gel column chromatography
3. customethyl acetate affords a compound still impure
4. washA second silica gel column chromatography eluting with 10:1 DCM