Content: Including objectives, methods adopted and literature review, around 2000 words
- Objectives
Medium rings are typically hard to make although they show many novel and important bioactivities. Based on former investigations, medium-ring keto lactams were found to have antimalarial activity. This project will aim at synthesizing compounds related to this structure. Chemical reaction mechanisms and preliminary structure-activity relationship (SAR) will also be studied.
- Methods Adopted
2.1 Compounds Preparation
2.1.1 beta;-Carboline compounds will be synthesized by applying the Pictet-Spengler Reaction. Tryptamine and tryptophan derivatives will be condensed with piperidones and benzaldehydes. TMSCl will function as the acidic catalyst while pyridine plays the role of solvent.
2.1.2 A combination of NaIO4 and formaldehyde using Witkop-Winterfeldt oxidation conditions will break the indole double bond and extend beta;-Carbolines into medium-sized ring systems.
2.2 Reactions Monitoring
Organic reactions usually take several hours to complete. GC/MS is widely deployed to trace the process of reactions, itrsquo;s more accurate in comparison with TLC. For molecules that are heat stable, GC/MS can also be utilized to test purity.
2.3 Structure Identification
In the field of chemistry and biology, nuclear magnetic resonance (NMR) spectroscopy is a sensitive tool to determine the structure and conformation of both small and large molecules. In this project, NMR will be frequently used to identify compound structures.
2.4 Products Purification
