No abstract

The synthesis of a novel D-ring modified docetaxel analogue, in which the oxetane ring is replaced with a γ-lactone, was achieved from 10-deacetylbaccatin III. The key steps of the synthesis include the direct acetylation of the secondary hydroxyl group at C-5 and D-ring opening and intramolecular aldol reaction to form the γ-lactone. In MTT assays, this analogue proved to have equipotent cytotoxicity relative to paclitaxel towards HCT8, HePG2 and BGC23 cancer cell lines, and be more potent than paclitaxel against A549 and A375. It represents the first example of D-ring modified taxoids with significant cytotoxicity.

No abstract

The title compound, C18H21NO3, was obtained via a double Mannich condensation reaction of 6-methyl­tetra­hydro­isobenzofuran-1,7(3H,7aH)-dione with formaldehyde and benzyl­amine. The mol­ecule contains three fused rings of which the cyclo­hexa­none and piperidine rings adopt chair conformations and the furan­one ring assumes an envelope conformation. An inter­molecular C—H⋯π inter­action is present in the crystal structure.

Aus dem Naphthalin (I) wird das Silylethinyl‐Derivat (V) hergestellt, das sich unter Katalyse des Cobalt‐Komplexes (VII) mit dem Acetylen (VI) zum Naphthalin (VIIIa) umsetzt.