An iridium-catalyzed ortho C-H borylation reaction directed by cyclic dithioacetal moiety is disclosed. A series of borylation products were obtained in moderate to good yields under mild conditions in exclusive mono- and ortho-regioselectivity. Thus, the 1,3-dithiane or 1,3-dithiolane group serves as a remarkable effective directing group for C-H borylation without any ligand assistance. The further transformations of the borylation products are also carried out to change boryl group to other functional groups.

Stereogenic osmium center mediates enantioselective ring-closing C(sp3)–H aminations of sulfonylazides and azidoformates.

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Carbene BÀ H insertion reactions represent an efficient method for CÀ B bond formation, which have experienced great advances in recent years. Free and metal carbene insertion into BÀ H bonds based on diazo and nondiazo carbene precursors, including α-diazoesters, α-diazoketones, hydrazones, chloroforms, acylsilanes, alkenyl triflates, alkynes and sulfoxonium ylides have been well studied. The development of this chemistry complements existing CÀ B bond formation strategies in terms of substrate scope, selectivity and product diversity. Notably, the catalytic enantioselective carbene BÀ H insertion reactions enable easy access to the challenging but important chiral organoboron compounds. This review provides a timely overview on this research topic. Typical achievements in reaction methodologies, plausible reaction mechanisms, as well as applications in the synthesis of bioactive molecules are summarized.

An efficient one-step synthesis of 2-acylquinolines by a copper-catalyzed tandem reaction of 2-ethynylanilines with glyoxals in the presence of piperidine has been developed. This new protocol successfully avoids the multi-step...