Discovery and Development of an Efficient Process to Atovaquone

…, C McCormick, CE Mountain, A Simpson…

Index: Britton, Hugh; Catterick, David; Dwyer, Andrew N.; Gordon, Andrew H.; Leach, Stuart G.; McCormick, Chris; Mountain, Clive E.; Simpson, Alec; Stevens, David R.; Urquhart, Michael W. J.; Wade, Charles E.; Warren, John; Wooster, Nick F.; Zilliox, Audrey Organic Process Research and Development, 2012 , vol. 16, # 10 p. 1607 - 1617

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Citation Number: 8

Abstract

The discovery and development of an efficient and more sustainable manufacturing route to the anti-pneumocystic agent atovaquone (2-((1 R, 4 R)-4-(4-chlorophenyl) cyclohexyl)-3- hydroxynaphthalene-1, 4-dione) 1 is described. The existing commercial route to atovaquone delivers a poor yield of product and uses expensive reagents. The new synthesis commences with readily available phthalic anhydride, which is converted to 1, 4 ...