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Paper | Regular issue | Vol 78, No. 1, 2009, pp.71-91
Published online, 28th August, 2008
DOI: 10.3987/COM-08-11482
Diversity-oriented Synthesis of Substituted Pyrazolo[4,3-d][1,2,3]triazin-4-ones

Daniel Meibom,* Marcus Bauser, Heinrich Meier, Dirk Schneider, Nils Svenstrup, and Dieter Haebich

*Medical Chemistry, Bayer Health Care AG, D-42096 Wuppertal, Germany


An efficient synthesis of 3,7-disubstituted 3,5-dihydro-4H-pyrazolo[4,3-d][1,2,3]triazin-4-ones (2), especially suited for late-stage decoration, is described. Diverse 3-benzyl analogs were obtained by amidation-cyclization in one pot and various pyrazolotriazinone-7-bromides were employed in Suzuki and Sonogashira cross-coupling reactions.