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Modafinil (2-[(diphenylmethyl)sulfinyl]acetamide, MOD) is a key psychostimulant drug used for the treatment of narcolepsy and other sleep disorders that has a very low addiction liability. Recently, MOD has been clinically investigated for the treatment of cocaine addiction and used by astronauts in long-term space missions. We have developed a synthetic strategy for “smart drug” Modafinil. An efficient atom and step economic (EASE) synthesis has been carried out by the direct reaction of benzhydrol and 2-mercaptoacetamide using the recyclable heterogeneous catalyst Nafion-H along with post-sulfoxidation. This protocol exhibits improved sustainability credentials. We have also developed a superior pre-sulfoxidation approach for the synthesis of Modafinil. [ABSTRACT FROM AUTHOR]

First in situ generation of a betaine intermediate has been developed using two new precursors oxobis(methylthio)ketene acetals and N-butyl-N′-methyl ethane-1,2-diamine for the synthesis of annulated dihydrofurans. This protocol adds a new dimension for the formation of annulated dihydrofurans through a series of selective consecutive formation of C–C and C–O bonds after reacting with enone rings. This in situ generated betaine intermediate corresponds to deoxy-Breslow intermediates in the reaction via elimination of NHC. [ABSTRACT FROM AUTHOR]