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Article / Mar 09, 2022

Monofluoromethylation of complex pharmaceutical steroids using non-depleting reagents

Authors:
  • Emilia P. T. Leitao
Source:
Research & Reviews: Journal of Pharmacy and Pharmaceutical Sciences (2022), 11(2), 27-34

Monofluoromethylated drugs are important but are less available. Common electrophilic monofluoromethylation methods are environmentally unsustainable; hence urgent solutions are required to advance in this field. Using a previously optimized protocol, in this paper, we are going to present the preparation of new non-depleting and low-cost monofluoromethylating reagents by replacing the benzene substitution. These reagents were successfully used in the synthesis of two important and complex steroids, Fluticasone propionate and Fluticasone furoate, pharmaceutical drugs for the treatment of asthma and rhinitis, resp.