Abstract
Propargylamines have been synthesized by a gold(III) salen complex-catalyzed three-component coupling reaction of aldehydes, amines, and alkynes in water in excellent yields at 40 °C. With chiral prolinol derivatives as the amine component, excellent diastereoselectivities (up to 99:1) have been attained. This coupling reaction has been applied to the synthesis of propargylamine-modified artemisinin derivatives with the delicate endoperoxide moieties remaining intact. Cytotoxicities with IC50 values up to 1.1 μM against a human hepatocellular carcinoma cell line (HepG2) were exhibited by these artemisinin derivatives.
Original language | English |
---|---|
Pages (from-to) | 1529-1532 |
Number of pages | 4 |
Journal | Organic Letters |
Volume | 8 |
Issue number | 8 |
DOIs | |
Publication status | Published - 13 Apr 2006 |
Externally published | Yes |
ASJC Scopus subject areas
- Biochemistry
- Physical and Theoretical Chemistry
- Organic Chemistry