The propargylation of various nucleophiles including indoles, phenol, anisole, enoxysilanes, and alcohols was rapidly achieved using catalytic copper(II) triflate. The reaction conditions are mild, allowing for quick reactions in an undried solvent and under atmospheric air. The desired products are obtained with good yields.

In order to obtain antibacterial candidate compounds, using the principle of pharmacodynamic fragment combination, the thiazole fragment was introduced into the structure of the seedling compound osthole. Twenty-six osthole derivatives were designed and synthesized, and confirmed by ¹H NMR, ¹³C NMR and elemental analysis. The antibacterial activities against S. aureus, E. coli, methicillin-resistant S. aureus (MRSA) and fluoroquinolone-resistant E. coli (FREC) were evaluated. The results showed that the minimum inhibitory concentrations (MICs) of N-(4-(2-fluorophenyl)thiazol-2-yl)-2-((8-(3-methyl- but-2-en-1-yl)-2-oxo-2H-chromen-7-yl)oxy)acetamide (5g) were 2, 4, 2, 4 μg/mL, respectively. The MICs of N-(4-cyclo- propylthiazol-2-yl)-2-((8-(3-methylbut-2-en-1-yl)-2-oxo-2H-chromen-7-yl)oxy)acetamide (5w) were 2, 2, 4, 4 μg/mL, respectively. The MICs of N-([2,4'-bithiazol]-2'-yl)-2-((8-(3-methylbut-2-en-1-yl)-2-oxo-2H-chromen-7-yl)oxy)acetamide (5x) were 1, 2, 2, 2 μg/mL. respectively. Their anti-S. aureu activities were comparable to the control drug oxacillin and superior to norfloxacin, and anti-E. coli, MRSA, and FREC were superior to the control drugs oxacillin and norfloxacin. The connection of thiazole fragment to the structure of osthole can effectively enhance antibacterial activities.

A more feasibly convergent synthesis of selective estrogen receptor degrading agent (S)-8-(4-((1-(3-fluoropropyl)- pyrrolidin-3-yl)oxy)phenyl)-7-(4-hydroxyphenyl)-5,6-dihydronaphthalen-2-ol was reported, featured with concise work up and absence of regioselectivity dilemma.

Normal-phase and reversed-phase silica gel column chromatography and semi-preparative high performance liquid chromatography were applied to study the chemical constituents of the stems and twigs of the Hainan mangrove plant, Excoecaria agallocha L. A new 3,4-seco-ent-kaurane diterpenoid, named agallochanin acid A (1), and a rare ent-tetranorlabdane diterpenoid, named agallochanin acid B (2), along with four known diterpenoids were isolated. Their structures including absolute configurations were characterized via HR-ESI-MS, extensive 1D and 2D NMR investigations and calculated and experimental electronic circular dichroism (ECD) data. All isolates were tested for their inhibitory effects on NO production in lipopolysaccharide (LPS)-activated BV-2 cells. ent-3,4-Seco-17-oxo-kaur-4(19),15(16)-dien-3-oic acid (3) and ent-15-hydroxy- labda-8(17),13E-dien-3-one (5) exhibited considerable anti-neuroinflammatory activities with IC₅₀ values of (14.32±1.99) and (4.24±0.37) μmol/L.

A Pd(OAc)₂-catalyzed efficient synthesis of 2-(1-isochromen-3-yl)acetaldehyde derivatives was achieved by the carboxyl-directed C—H bond alkylation/annulation of aryl acids with vinyl ethylene carbonate. This method has the advan- tages of ready availability of starting materials and operational simplicity, providing an alternative access to isochroman-1-one derivatives.