|
|||||
|
|
Synthesis and biological evaluation of a des-dihydropyran laulimalide analog |
|
| Authors: | Andreas Gollner Karl-Heinz Altmann Jürg Gertsch Johann Mulzer |
| Institution: | aInstitute of Organic Chemistry, University of Vienna, Währingerstrasse 38, 1090 Vienna, Austria;bInstitute of Pharmaceutical Sciences, ETH Zürich, Wolfgang-Pauli-Strasse 10, 8093 Zürich, Switzerland;cInstitute of Biochemistry and Molecular Medicine, Universtiy of Bern, Bühlstrasse 28, 3012 Bern, Switzerland |
| Abstract: | The preparation of a novel simplified Laulimalide analog via a highly convergent and efficient route and its biological evaluation are presented. The outlined route enables the synthesis of C5–C9 modified analog 2 and uses Julia–Kocienski olefination for fragment assembly and a regioselective Yamaguchi macrolactonization for ring closure. This strategy should be suitable for the generation of various new C5–C9 des-dihydropyran laulimalide derivatives for further SAR studies. |
| Keywords: | Antitumor drugs Total synthesis SAR studies Evans alkylation Macrolactonization |
| 本文献已被 ScienceDirect 等数据库收录！ | |