A transition-metal-free method for the construction of functionalized quinolines from readily available acetophenones and anthranils is reported. This one-pot reaction cascade involves in situ generation of α,β-unsaturated ketones from the acetophenone via one-carbon homologation by DMSO followed by the aza-Michael addition of anthranils and subsequent annulation. DMSO acted in this reaction not only as solvent but also as one carbon source, thus providing a highly atom-economical and environmentally benign approach for the synthesis of 3-substituted quinolines.

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We herein report hydrazine-directed, Rh(III) catalyzed (4+2) annulation of N-alkyl aryl hydrazines with sulfoxonium ylides as a safe carbene precursor. The reaction shows excellent functional group tolerance with broad substrate...

Carboxylic acids are ubiquitous functional groups present in many bio-relevant molecules, including drugs and amino acids. In general, αand βÀ C(sp 3 )À H bonds of carboxylic acids are easy to functionalize, contrary to remote (γ-and δ) CÀ H bonds which are difficult due to the distal location of these CÀ H bonds from the functional group. On the other hand, functionalizing an inert C(sp 3 )À H bond is another critical challenge in synthetic chemistry due to its lower acidity and reactivity. Nevertheless, the last decade has witnessed tremendous development in remote sp 3 -CÀ H bond functionalization of carboxylic acid and its derivatives. Here, in this review, we have delineated recent progress in remote γand δ-CÀ H bond functionalization of aliphatic carboxylic acids/amino acids and their derivatives. This review is further subdivided based on the type of functionalization reaction. Finally, we have presented some applications of these methodologies, such as total synthesis of hibispeptin A, etc.