Zileuton chemistry

Benzothiophenes have always been of interest for medicinal chemistry and can be found in a number of marketed drugs such as Sertaconazole (Gineder-mofix), Zileuton (Leutrol) and Raloxifene (Evista). The classical synthesis of benzo thiophenes starts from thiophenols, reacting with bromoacetaldehyde dimethyl acetal, followed by cycUzation using strong acid. An alternative and more convenient route was also described starting from benzaldehydes which... 

The importance of thiophenes in medicinal chemistry can be highlighted by the enormous economic success of thiophene-containing drugs. Pharmaceuticals containing thiophenes such as duloxetine (Cymbalta), olanzapine (Zyprexa), tiotropium (Spiriva), raloxifene (Evista), and zileuton (Zyflo) had combined sales of more than 6 billion in the U.S. in 2010, while the blockbuster drug clopidogrel (Plavix) alone obtained sales in excess of 6 billion in the same year. 

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