- Synthesis and Functionalization of C6/C7 Substituted Pyrido[3,2-d]pyrimidines
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An efficient synthesis of functionalized pyrido[3,2-d]pyrimidines is reported. Starting from 4-aminopyrimidine-3-carbaldehydes, a Horner-Wadsworth-Emmons olefination followed by a photoisomerization/cyclization installed the fused pyridine ring. Using substituted HWE-reagents various substituents could be introduced in the 7-position of the pyrido[3,2-d]pyrimidines. Functionalization of the pyridone substructure allowed late variation in the 6-position. In order to obtain amine-linked bis-pyridopyrimidines, 7-bromo-pyridopyrimidines were converted with their 7-amino-counterpart by Hartwig–Buchwald amination.
- Hofmann, Philipp E.,Meinecke, Jannick,Harms, Klaus,Koert, Ulrich
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- Pyrimido [5, 4-d] pyrimidines, pharmaceuticals containing these compounds, their use and processes for their preparation
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Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of oncoses, and their preparation. Exemplary compounds are: (a) 4-(5-indolylamino)-6-morpholinopyrimido[5,4-d]pyrimidine; (b) 4-(5-indolylamino)-6-[trans-(4-hydroxycyclohexyl)amino]pyrimido[5,4-d]pyrimidine; (c) 4-[(3-chloro-4-fluorophenyl)amino]-6-[4-(morpholinocarbonylmethyl)-1-piperazinyl]pyrimido[5,4-d]pyrimidine; (d) 4-[(3-chloro-4-fluorophenyl)amino]-6-[(4-morpholinyl)amino]pyrimido[5,4-d]pyrimidine; (e) 4-[(3-chloro-4-fluorophenyl)amino]-6-(4-picolylamino)pyrimido[5,4-d]pyrimidine; (f) 4-[(3-chloro-4-fluorophenyl)amino]-6-[1-trifluoroacetyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine; (g) 4-[(3-chloro-4-fluorophenyl)amino]-6-(endo-tropinylamino)pyrimido[5,4-d]pyrimidine; and, (h) 4-[(3-chloro-4-fluorophenyl)amino]-6-(exo-tropinylamino)pyrimido[5,4-d]pyrimidine.
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- Pyrimido?5,4-D!pyrimidines, medicaments comprising these compounds, their use and processes for their preparation
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The present invention relates to pyrimido?5,4-d!pyrimidines of the general formula STR1 in which Ra to Rc are as defined herein, their tautomers, their stereoisomers and their salts, in particular their physiologically tolerated salts with inorganic or organic acids or bases which have valuable pharmacological properties, in particular an inhibiting action on signal transduction mediated by tyrosine kinases, their use for the treatment of diseases, in particular tumor diseases.
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- Pyrimido[5,4]-dipyrimidines, pharmaceuticals containing them, their use and processes for the preparation thereof
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Pyrimido[5,4-d]pyrimidines of the general formula [Figure] which have an inhibitory effect on signal transduction mediated by tyrosine kinases, their use for the treatment of disorders, in particular of oncoses, and their preparation. Exemplary compounds are: 4-[(3-Chloro-4-fluorophenyl)amino]-6-[1-methyl-4-piperidinylamino]pyrimido[5,4-d]pyrimidine, and 4-[(3-Chloro-4-fluorophenyl)amino]-6-[trans-4-dimethyl-aminocycohexylamino]pyrimido[5,4-d]pyrimidine.
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