A novel approach to the synthesis of diaza-bridged heterocycle derivatives |
| |
Authors: | Isabel M Gomez-Monterrey Alessia Bertamino Maria V Diurno Paolo Grieco |
| |
Institution: | a Department of Pharmaceutical and Toxicological Chemistry, University of Naples ‘Federico II’, I-80131 Naples, Italy b Department of Pharmaceutical Science, University of Salerno, I-84084 Fisciano, Italy |
| |
Abstract: | A novel synthetic route of diaza-bridged heterocycles based on natural 3,9-diazabicyclo3.3.1]non-6-ene scaffold has been accomplished. The synthetic approach consists of a Pictet-Spengler condensation of the l-Dopa-OMe with an appropriate aldehyde, Fmoc-Aa-H, followed by intramolecular lactamization. This approach generated two configurationally distinct products (cis and trans-isomers), increasing the stereochemical diversity of these compounds. The synthesized compounds are potentially useful in the discovery of novel pharmacologically active compounds. |
| |
Keywords: | Amino acids Intramolecular cyclization Molecular diversity Antitumor agents |
本文献已被 ScienceDirect 等数据库收录! |
|