Single pot conversion of artemisinin into arteether
AssigneeCouncil of Scientific and Industrial Research
InventorsRajendra Singh Bhakuni, Amit Tewari, Tarun Singh, Suman P.S. Khanuja
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Abstract
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.
Claims22
A single pot process for the preparation of arteether from artemisinin comprising the steps of:
- (a) dissolving artemisinin and a polyhydroxy catalyst in ethanol at room temperature to obtain a solution,
- (b) adding a reducing agent to step (a) solution, stirring the reaction mixture at a temperature ranging between 20 to 30° C. for about 0.5 to 2 hours to reduce artemisinin into dihydroartemisinin,
- (c) adding an acid catalyst to the reaction mixture of step (b) with cooling,
- (d) stirring the reaction mixture of step (c) for about 1 to 2 hours at room temperature,
- (e) adding cold water to the reaction mixture of step (d), extracting with a mixture of ethyl acetate and n-hexane, separating the organic layer,
- (f) washing the organic layer of step (e) with 0.5% aqueous sodium bicarbonate solution followed by water,
- (g) drying the washed organic layer of step (f) over anhydrous sodium sulphate, filtering, evaporating the organic layer to obtain a residue, and
- (h) purifying the residue of step (g) by silica gel column chromatography to obtain arteether.
Dependencies are inferred from the claim text.