An Improved and Scalable Process for Zafirlukast: An Asthma Drug

Abstract

An improved and scalable process for the large-scale production of zafirlukast (Accolate), an important drug for asthma, is discussed along with impurity and scale-up-related issues.

Large-Scale Applications of Amide Coupling Reagents for the Synthesis of Pharmaceuticals

“…The application of DCC for amide bond formation is showcased in the numerous reports from pharmaceutical companies. ,,, Despite being a strong sensitizer, its low cost is one of the main drivers for its widespread use.…”

Visible light-mediated C P bond formation reactions

“…No external oxidants are needed for the process documenting the redox neutral character of the reaction. Furthermore, the synthetic value of the method is highlighted by the formal synthesis of Zafirlukast derivative, an oral leukotriene receptor antagonist for the maintenance treatment of asthma [83]. A series of control experiments suggested a reductive quenching process of this process.…”

Novel zafirlukast derivatives exhibit selective antibacterial activity againstPorphyromonas gingivalis

“…Several synthetic methods were reported for either linear or convergent synthesis of zafirlukast. 29,30,[33][34][35][36][37][38][39] Here, the concise and linear synthesis of zafirlukast derivatives involved C-C bond formation between various substituted indoles and benzoyl analogues followed by a subsequent sulfamidation step. The initial synthesis centered on creating zafirlukast derivatives 4a and 4b with variations in the arylsulfonamide domain as well as the elimination of the cyclopentyl carbamate of the indole of the parent molecule (Scheme 1).…”