Acedapsone Synthesis
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Acedapsone ( INN) is an antimicrobial drug, which also has antimalarial activity. Acedapsone is the INN for diacetyl
dapsone Dapsone, also known as 4,4'-sulfonyldianiline (SDA) or diaminodiphenyl sulfone (DDS), is an antibiotic commonly used in combination with rifampicin and clofazimine for the treatment of leprosy. It is a second-line medication for the treatment a ...
. It was synthesized and developed in 1937 by
Ernest Fourneau Ernest Fourneau (4 October 1872 – 5 August 1949) was a French pharmacist graduated in Pharmacy 1898 for the Paris university specialist in medicinal chemical and pharmacology who played a major role in the discovery of synthetic local anesthetic ...
and his team in the pharmaceutical chemistry laboratory of Pasteur Institute, and it was marketed as Rodilone by the Rhône-Poulenc company. It is a long-acting
prodrug A prodrug is a medication or compound that, after intake, is metabolized (i.e., converted within the body) into a pharmacologically active drug. Instead of administering a drug directly, a corresponding prodrug can be used to improve how the drug ...
of dapsone. It is used for treating leprosy. It crystallises as pale yellow needles from diethyl ether, and as leaflets from dilute ethanol. It is slightly soluble in water.


Synthesis

Acedapsone is conveniently prepared by acetylation of dapsone.


References

Benzosulfones Withdrawn drugs Antileprotic drugs {{antimicrobial-stub