- A concise regioselective synthesis of hydroxyazaisoindolinones and their conversion into pyridopyridazinones
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The synthesis of pyridopyridazinones 7 and 8 via the reaction of hydroxyazaisoindolinones 5 and 6 with hydrazine hydrate is described. Compounds 7 and 8 were then subjected to reactions with alkyl halides to furnish N-alkyl derivatives. Only in the reaction of pyridopyridazinone 8 with benzyl bromide was the O-benzylpyridopyridazine 14b formed in addition to the N-benzylpyridopyridazinone 14a.
- Brzezinski, Jacek Z.,Bzowski, Henryk B.,Epsztajn, Jan
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- Synthesis of Some Novel N-Substituted Phthalazinone and Pyridopyridazinone Derivatives
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Phthalazinone and pyridopyridazinone derivatives 3, 5, and 9 were prepared via reaction ofappropriate lactams 2 and 8 with 2-bromoethylphthalimide, N-tosylaziridine, and N,O-ditosyl derivatives of N-methylethanolamine in a two-step process in the presence
- Malinowski, Zbigniew,Sroczyński, Dariusz,Szczes?niak, Aleksandra K.
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p. 1743 - 1750
(2015/08/06)
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- Tetrahydropyrido[d]pyridazinones - Promising scaffolds for drug discovery
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An approach to the synthesis of all possible tetrahydropyrido[d] pyridazinones has been developed. The method relies on the catalytic hydrogenation of the corresponding aromatic counterparts, which were obtained by cyclization of the relevant dibromomethyl-substituted pyridinecarboxylates with hydrazine. The synthetic schemes include 4-5 steps starting from commercially available materials. The tetrahydropyrido[d]pyridazinone scaffolds are combinations of a saturated heterocycle (piperidine) and a privileged aromatic heterocycle (pyridazinone); hence they are promising starting points for the design in medicinal chemistry.
- Yaremenko, Anatoliy G.,Volochnyuk, Dmitriy M.,Shelyakin, Vyacheslav V.,Grygorenko, Oleksandr O.
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p. 6799 - 6803
(2013/07/26)
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- Synthesis and pharmacological evaluation of N- (dimethylamino)ethyl derivatives of benzo- and pyridopyridazinones
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New N-(dimethylamino)ethyl derivatives of phthalazinones and pyridopyridazinones 7, 9 were synthesized and assayed as potential analgesic agents in the hot-plate, tail-flick, and writhing tests. Pharmacological assay demonstrated that eight (in ten) of th
- Pakulska, Wanda,Malinowski, Zbigniew,Szczesniak, Aleksandra K.,Czarnecka, Elzbieta,Epsztajn, Jan
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scheme or table
p. 41 - 47
(2009/06/06)
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