A practical and mild strategy has been developed for the selective O-arylation on C-6 substituted pyridin-2-ones with a series of arylboronic acids, using Cu(OTf)2 as the catalyst, DABCO as the ligand, Et3N as the base, and K2HPO4 as the additive. This method affords O-arylated pyridin-2-ones with good selectivity and yields

A series of novel \(N\)-(3,4,5-trimethoxyphenyl)pyridin-2(\(1H\))-one derivatives were designed, synthesized, and evaluated for their in vitro cytotoxicity against human colon cancer cells HCT-116. The key steps involved consecutive Chan–Lam- and Buchwald–Hartwig couplings. Most of these C-6 substituted pyridone derivatives showed moderate antiproliferative activity. The preliminary SAR indicated that the conformationally restricted pyridones exhibited more potent cytotoxicity than the flexible counterparts. In addition, cell cycle analysis of the selected compounds 4b and e showed a G2/M arrest, suggesting a possible antitubulin mechanism for these novel pyridone derivatives.

A new synthetic method for phosphatidylethanolamine head group was developed via ring-opening of cyclic dioxaphospholane 2 with sodium azide and subsequent hydrogenation. The advantage of this strategy included short reaction steps, readily available materials and good yields.

A new practical and concise total synthesis of enantiopure camptothecin and SN-38 (14% overall yield, 99.9% ee and 99.9% purity) was described, starting from inexpensive and readily available materials. The development of column chromatography-free purification was achieved in all steps, which offers an economic industrial process to the camptothecin-family alkaloids.

Several 7-alkynyl camptothecin derivatives were prepared via Sonogashira coupling. And anti-tumor activities of these compounds were evaluated against human esophageal cancer cell line (Eca-109), human chronic myeloid leukaemia cell line (K562), bladder cancer cell line (5637) and gastric cell line (SGC7901). Compounds 9a–d and 10a exhibited remarkable in vitro cytotoxic activity, compared with topotecan.