As one of the most versatile intermediate group in synthetic chemistry, the introduction of an aldehyde group into a specific moiety is important for the transformation of molecular structures. Herein, we provided a metal-free, regioselective and one-pot formylation of the indolo[2,1a]isoquinoline moiety. This strategy features an oxidative coupling process using commercially available 1,3-dioxolane as a formylated reagent followed by direct hydrolyzation without a separation process. This reaction can be carried out under common reaction conditions and displays broad functional group tolerance.

A new briarane-type diterpenoid, briaviolide Q (1), along with a known analogue, excavatolide Z (2), were obtained from a cultured octocoral Briareum violaceum. Details of the isolation and structure determination of briarane 1 from spectroscopic data are presented in this paper. In RAW264.7 cells, a macrophage-like murine cell line, briarane 1 was found to inhibit the protein expression of pro-inflammatory inducible nitric oxide synthase (iNOS) in cells stimulated by lipopolysaccharide (LPS).

A metal‐free radical relay addition/cyclization of activated alkenes with ethers, cycloalkanes, toluenes, and alcohols has been achieved, leading to a range of functionalization of 5,6‐dihydrobenzo[4,5]imidazo[2,1‐a]isoquinolines with the yield of 43% ‐ 84%. This protocol exhibits advantages of metal‐free, base‐free, and shorter reaction time.

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