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One-Step Continuous Flow Synthesis of Antifungal WHO Essential Medicine Flucytosine Using Fluorine

By Harsanyi, Antal; Conte, Annelyse; Pichon, Laurent; Rabion, Alain; Grenier, Sandrine; Sandford, Graham

Published on

Abstract

In Africa around 625 000 mortalities per annum (20% of HIV/AIDS related deaths) are due to the affects of the Cryptococcal meningitis (CM) fungal infection. Recently, the World Health Organisation (WHO) and the Infectious Disease Society of America (IDSA) recommended that the first line treatment for CM is a combination of amphotericin B and flucytosine, both now WHO Essential Medicines. However, flucytosine is not even registered for use in any African nation due, in part, to its relatively high cost of manufacture and lack of generic manufacturers. Currently, flucytosine is manufactured by an expensive four-step manufacturing process. Here we report a one-step continuous flow process involving the reaction of inexpensive cytosine with fluorine gas using stainless steel tubular laboratory and pilot-scale silicon carbide reactor devices which is readily scaleable to a manufacturing process with a low initial capital expenditure.

Journal

Organic Process Research & Development. Volume 21, 2017, 273–276

DOI

10.1021/acs.oprd.6b00420

Type of publication

Peer-reviewed journal

Affiliations

  • Durham University
  • Sanofi Aventis
  • Maison Européenne des Procédés Innovants (MEPI)

Article Classification

Research Article

Classification Areas

  • API

Tags