Single pot conversion of artemisinin into arteether

Details Single pot conversion of artemisinin into arteether Single pot conversion of artemisinin into arteether

C - Chemistry, Metallurgy

07

D

C07D 493/22 (2006.01) C07D 307/92 (2006.01) C07D 493/18 (2006.01)

Patent

CA 2507078

The present invention provides a method for the preparation of arteether from artemisinin in one pot in just about 4 hours comprising reduction of artemisinin into dihydroartemisinin by less quantity of sodium borohydride in ethanol at room temperature in the presence of a novel polyhydroxy catalyst, acylation of dihydroartemisinin in the presence of an acid catalyst, extraction of arteether from an aqueous reaction mixture using 1% ethyl acetate in n-hexane followed by workup and purification of the impure arteether to yield 80-86% (w/w) pure alpha, beta arteether.

L'invention porte sur un procédé de préparation d'artééther à partir d'artémisinine, en four monocellulaire et en seulement environ 4 heures, comportant les étapes suivantes: réduction de l'artémisinine en dihydroartémisinine par une petite quantité de borohydrure de sodium dans de l'éthanol, à température ambiante, et en présence d'un nouveau catalyseur polyhydroxy; acylation de la dihydroartémisinine en présence d'un catalyseur acide; extraction de l'artééther d'un mélange réactif aqueux à 1 % d'acétate d'éthyle dans du n-hexane, suivie d'un traitement conclusif; et purification de l'artééther impur donnant des artééthers alpha et bêta à 80-86 % (en poids) de pureté.

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