ChemicalBook CAS DataBase List Artesunate

Artesunate synthesis

4synthesis methods

Product Name:Artesunate
CAS Number:88495-63-0
Molecular formula:C19H28O8
Molecular Weight:384.42

Artemisinin was discovered in the 1970s as a result of an extensive screening of Chinese herbal extracts in the search of new antimalarial agents. Currently, the primary method for the production of artemisinin is the isolation from dried leaves of the plant Artemisia annua. Furthermore, the global supply of this life-saving drug exclusively from natural sources remains highly limited. As a result, a novel approaches for large-scale production of artemisinin have been developed. Artesunate is prepared from dihydroartemisinin (DHA) by reacting it with succinic acid anhydride in a basic medium.

A simplified and scalable synthesis of artesunate

108-30-5 Synthesis

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81496-81-3 Synthesis

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88495-63-0
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Yield:88495-63-0 97%

Reaction Conditions:

with dmap in 1,2-dichloro-ethane at 45; for 6 h;Industrial scale;Reagent/catalyst;Solvent;Temperature;

Steps:

1

Weigh 5 kg of dihydroartemisininIn the jacketed stainless steel reactor R1,Adding 50.0 L dichloroethane,Room temperature stirring dissolved,To prepare a solution; weigh the succinic anhydride 10kg in a jacketed stainless steel reactor R2, add 40.0L dichloroethane, add 50g DMAP, stirring at room temperature, made of solution;The solution in the reactor R1 was added dropwise to the reactor R2 for 4 hours and the mixture was stirred for 2 hours. The pH of the reaction solution was adjusted to 5 with hydrochloric acid and concentrated to a solvent-free solution. 25L dichloroethane and 25L water, stirring extraction, liquid separation, 25L dichloroethane repeated extraction time;The organic phases were combined, dried over anhydrous sodium sulfate, fine filtered, concentrated under reduced pressure,Artesunate 6.56 kg,Yield 97.0%HPLC detection purity 99.9%

References:

CN106946904,2017,A Location in patent:Paragraph 0030; 0031

108-30-5 Synthesis

108-30-5
609 suppliers
$5.00/25g