Process for preparing n-substituted hydroxypyrimidinone...

Details Process for preparing n-substituted hydroxypyrimidinone... Process for preparing n-substituted hydroxypyrimidinone...

C - Chemistry, Metallurgy

07

D

C07D 239/52 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2710987

Processes for preparing certain N-arylalkyl-1-(alkyl or aralkyl)-2-acylaminoalkyl- 5-hydroxy -6-oxo-1,6-dihydropy- rimidine-4-carboxamides are disclosed. In one embodiment, the process comprises acylating the free amine in the corresponding N-arylalkyl-1-(alkyl or aralkyl)- 2-aminoalkyl-5-ester protected hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide and then deprotecting the 5-hydroxy by base hydrolysis. The hydroxypyrim- idinone carboxamide products of the process are HTV integrase inhibitors which are useful for treating HTV infection, treating AIDS, or delaying the onset or progression of AIDS. Certain esterified N-arylalkyl hydroxypyrimidinone carboxamides that can be employed as process intermediates are also disclosed.

L'invention concerne des procédés de préparation de certains N-arylalkyl-1-(alkyl ou aralkyl)-2-acylaminoalkyl-5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamides. Selon un mode de réalisation, le procédé comprend l'acylation de l'amine libre dans l'hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide protégé par leN-arylalkyl-1-(alkyl ou aralkyl)-2-aminoalkyl-5-ester correspondant, puis la déprotection du 5-hydroxy par hydrolyse basique. Les produits hydroxypyrimidinone carboxamide du procédé sont des inhibiteurs de VIH intégrase qui sont utiles pour le traitement de l'infection par le VIH, pour le traitement du SIDA ou pour retarder l'apparition ou la progression du SIDA. L'invention concerne également certains N-arylalkyl hydroxypyrimidinone carboxamides estérifiés qui peuvent être employés en tant qu'intermédiaires de procédé.

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