Abstract
An expedited approach to the synthesis of fused-dihydropyrazin-2(1H)-ones from Ugi dimethylacetamide adducts is presented. The protocol relies on the formation of a C–N bond between the primary amide and the transitory oxocarbenium ion formed under acidic conditions, and then the construction of a fused-pyrazinone system after an intramolecular C(sp2)-C(sp2) Heck coupling. The methodology was able to generate 21 structurally diverse poly aza-heterocycles, a collection which was screened for its cytotoxicity in prostate, breast and lung cancer cell lines. The best activity was observed against the prostate cancer cell line PC-3 for two compounds with IC50 values of 23.6 and 20.9 μM, respectively.
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