The synthesis of tetrahydropyridopyrimidones as a new scaffold for HIV-1 integrase inhibitors

Author:

Kinzel Olaf D.,Monteagudo Edith,Muraglia Ester,Orvieto Federica,Pescatore Giovanna,Ferreira Maria del Rosario Rico,Rowley Michael,Summa Vincenzo

Publisher

Elsevier BV

Subject

Organic Chemistry,Drug Discovery,Biochemistry

Reference13 articles.

1. 4,5-Dihydroxypyrimidine Carboxamides and N-Alkyl-5-hydroxypyrimidinone Carboxamides Are Potent, Selective HIV Integrase Inhibitors with Good Pharmacokinetic Profiles in Preclinical Species

2. Crescenzi, B.; Kinzel, O.; Muraglia, E.; Orvieto, F.; Pescatore, G.; Rowley, M.; Summa, V. A preparation of tetrahydro-4H-pyrido[1,2-a]pyrimidine derivatives, useful as HIV integrase inhibitors. WO 2004058757 A1.

3. Similar bicyclic pyrimidone structures with a heteroatom in the saturated ring have been described in a recent patent. Naidu, B. N.; Banville, J.; Beaulieu, F.; Connolly, T. P.; Krystal, M. R.; Matiskella, J. D.; Ouellet, C.; Plamondon, S.; Remillard, R.; Sorenson, M. E.; Ueda, Y.; Walker, M. A. Bicyclic heterocycles as HIV integrase inhibitors. WO 2007064316 A1.

4. Highly selective synthesis of 2-substituted-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxylic acid derivatives using a novel protected dihydroxyfumarate

5. Synthesis of 5,6-dihydroxy-2-phenyl-4-pyrimidinecarboxylic acid, methyl ester, a corrected structure

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