Two 1‐[6]helicenol derivatives were synthesized by Ni‐catalyzed [2+2+2] cycloaddition on a multigram scale. Both enantiomers of the 1‐[6]helicenols could be efficiently prepared by simple optical resolution. As a synthetic application of helically chiral 1‐[6]helicenols, a novel class of [6]helicene‐based phosphinites was developed; these compounds represent the first examples of helically chiral phosphinite ligands. Up to 90 % ee was obtained for the Pd‐catalyzed asymmetric allylic alkylation reaction.

A new class of solution-processable thieno[3,2-f:4,5-f′]bis[1]benzothiophene (TBBT-V) semiconductors are facilely synthesized and fully investigated.

The first enantioselective Pictet–Spengler reaction of acyclic α-ketoesters with tryptamines has been developed. Excellent yields and enantioselectivity were obtained for the reaction using chiral imidazoline-phosphoric acid catalysts. Density functional theory calculations suggested possible transition states that explain the origin of chiral induction. This process provides an efficient route for the synthesis of tetrahydro-β-carboline derivatives.

We designed and synthesized a novel 1,2-deoxy-pyranose and terminal epoxide methyl substituted derivatives of spliceostatin A using Julia–Kocienski olefination as a key step. With respect to the biological activity, the 1,2-deoxy-pyranose analogue of spliceostatin A suppressed AR-V7 expression at the nano level (IC50 = 3.3 nM). In addition, the in vivo toxicity test showed that the 1,2-deoxy-pyranose analogue was able to avoid severe toxicity compared to spliceostatin A.