A GREENER APPROACH TO SYNTHESIS OF DIACEREIN

摘要

Diacerein, also known as diacetylrhein (1,8-diacetoxy-3-carboxyanthraquinone), is a slow-acting active pharmaceutical ingredient of the anthraquinone class used to treat joint diseases such as osteoarthritis (swelling and pain in the joints). It works by inhibiting interleukin-1 beta and demonstrates anti-arthritic activity without inhibiting prostaglandin synthesis. Diacerein-containing medications are registered in some European Union and Asian countries and are included as a treatment option on several international therapeutic guidelines. Different approaches have been reported for the synthesis of this compound. Many approaches have been reported for preparation of diacerein specially employing reagents like hexavalent chromium compounds which are toxic and effluent-unfriendly. We report herein synthesis of diacerein, a potent antiarthritic ingredient, by employing a greener chemical method and also synthesis of acetyl vanillic acid by employing similar scheme having same functional groups.