Process for the preparation of abacavir

Details Process for the preparation of abacavir Process for the preparation of abacavir

C - Chemistry, Metallurgy

07

D

C07D 473/16 (2006.01)

Patent

CA 2662586

Process for removal of the amino protective group of a N-acylated {(1S,4R)-4- [2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}methanol of formula (II) where R = H or a (C1-C4)-alkyl, using an inorganic base in a mixture of water and alcohol, to yield abacavir or its salts. The process proceeds very fast and the product can be obtained in high yield and purity.

L'invention porte sur un procédé d'élimination du groupe amino protecteur d'un (1S,4R)-4- [2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-cyclopent-2-enyl}méthanol N-acylé de formule (II) dans laquelle: R = H ou (C1-C4)-alkyle, en utilisant une base minérale dans un mélange d'eau et d'alcool pour obtenir l'abacavir ou ses sels. Le procédé est très rapide et permet d'obtenir un rendement et une pureté élevés.

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