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 473/00 (2006.01)

Patent

CA 2670432

Process for the preparation of abacavir, or its salts or its solvates comprising the step of reacting a compound (IV) where R1 is a (C1-C 4)-alkyl radical with anhydrous hydrochloric acid/(C1-C6)-alcohol, and then with tri(C1-C 4)-alkyl orthoformate, in the absence of water. The preparation process may include further steps of reacting the compound obtained with cyclopropylamine and subsequently hydrolysis to yield abacavir.

L'invention concerne un procédé pour la préparation d'abacavir, de ses sels ou de ses solvates, comprenant l'étape consistant à faire réagir un composé (IV) dans lequel R1est un radical alkyle en C1-C4 avec de l'acide chlorhydrique anhydre/alcool en C1-C6, puis avec un orthoformiate de tri-alkyle en C1-C4 en l'absence d'eau. Le procédé de préparation peut comprendre d'autres étapes de réaction du composé obtenu avec de la cyclo-propylamine et d'hydrolyse ultérieure pour donner l'abacavir.

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