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Present work reports a novel and commercially viable method for the synthesis of 2-chloro-3-[trans-4-(4-chlorophenyl) cyclohexyl]-1,4-naphthoquinone 1, a renowned intermediate of Atovaquone (an antimalarial drug). Majority of the prior arts disclose the synthesis of this intermediate from the expensive starting material 2-chloro-1,4-naphthoquinone 2, in relatively low yield. In this regard, it was considered worthwhile to synthesize 1 by a novel route using cheaper starting material 2,3-dichloro-1,4-naphtoquinone 5, in high yield and purity. In the present study, emphasis was given for selecting the reagents and solvents, optimizing the reaction conditions, recovery and reuse of solvents and silver salt. This optimized novel process is cost effective and generate less effluents.

Present study involves the synthesis, characterization, antimalarial and anticancer activities of some novel substituted amino analogues of 1,4-naphthoquinone. The chloro group present in the key starting materials like 2,3-dichloro-1,4-naphthoquinone (1) and 2-chloro-3-[trans-4-(4-chlorophenyl)- cyclohexyl]-1,4-naphthoquinone (2) was replaced by substituted amines. These analogues were isolated, purified and screened for antimalarial and anticancer activities. A few of the novel compounds were found to possess substantial biological activity and are reasonably potent.

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