Process for the preparation and purification of...

C - Chemistry – Metallurgy – 07 – C

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C07C 67/343 (2006.01) C07C 69/738 (2006.01)

Patent

CA 2531059

In its several embodiments, this invention discloses a novel process to prepare the compounds of Formula 3, wherein R1 is lower alkyl, and R2 and R3 can be the same or different, each being independently selected from the group consisting of alkyl, aryl and aralkyl; said process being carried out in a suitable solvent with at least one tert-amine carboxylate salt catalyst. The compounds of formula 3 are chemical intermediates useful for the synthesis of various heterocyclic compounds. These heterocyclic compounds are in turn useful precursors for diverse pharmaceutical, herbicidal and insecticidal agents. In particular, these intermediates are useful precursors to a variety of CCR5 inhibitors.

Dans plusieurs modes de réalisation, cette invention concerne un nouveau processus de préparation des composés de formule 3. Dans ladite formule, R?1¿ représente un alkyle inférieur, et R?2¿ et R?3¿ peuvent être identiques ou différents, chacun étant sélectionné indépendamment parmi le groupe englobant un alkyle, un aryle et un aralkyle, ledit procédé étant réalisé dans un solvant approprié avec au moins un catalyseur de sel de carboxylate de tert-amine. Lesdits composés de la formule 3 sont des intermédiaires chimiques utilisés dans la synthèse de divers composés hétérocycliques. Ces composés hétérocycliques sont, à leur tour, utilisés comme précurseurs de plusieurs agents pharmaceutiques, herbicides et insecticides. Notamment, ces intermédiaires sont utilisés comme précurseurs avec divers inhibiteurs CCR5.

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