Process for preparation of atovaquone and novel intermediates thereof
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United States of America Patent
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Dec 7, 2010
Grant Date -
Apr 1, 2010
app pub date -
Oct 21, 2009
filing date -
Apr 19, 2007
priority date (Note) -
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Abstract
Disclosed herein is a novel process for preparation of atovaquone. The process includes reacting 1,4-naphthoquinone with trans-4-(4-chlorophenyl) cyclohexane carboxylic acid followed by halogenation to obtain a dihalo-compound. Further, dehydrohalogenation of the dihalo-compound produces a monohalogeno-compound which under goes hydrolysis to produce atovaquone. The invention also discloses atovaquone in a substantially pure and well defined polymorphic form designated as “Form IPCA-ATO,” and the preparation thereof.
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