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15th July 2015 @ 11:54

Hi,

I’m Tianyi, currently an exchange student from Nanjing University. I’ll be in Mat’s group for two months and now I am doing some chemistry on the Open Source Malaria project with Alice in lab.

My work mainly focuses on the construction of the MMV669846, which has one less nitrogen in its core structure compared to other molecules. This molecule is promising because it’s biological active against malaria and has improved metabolism. The construction and modification of its core structure is the key to the whole synthesis of this kind of compound.

The first task is to develop new methods for core synthesis.

For modification of the core structure, that is to substitute the hydrogen on 3-position, we’ll develop new methods on bromination chemistry so that we can functionalise the core structure further. We’ll start with 5-chloro-[1,2,4]triazolo[4,3-a]pyrazine as a model.

Our third task is to replace the hydrogen connected to 2-position carbon with groups like methyl etc. We do this in order to improve metabolism of the compound on one hand and to use the substituent group as a handle to attach the compound to the surface of solid on the other hand. We'll start with 5-chloroimidazo[1,2-a]pyrazine.

 

Finally, we’ll see if we can synthesise a functionalised core in only one step.

Attached Files
5-chloro-[1,2,4]triazolo[4,3-a]pyrazine.cdxml
5-chloro-[1,2,4]triazolo[4,3-a]pyrazine.png
5-chloro-3-phenylimidazo[1,2-a]pyrazine.cdxml
5-chloroimidazo[1,2-a]pyrazine.cdxml
5-chloro-3-phenylimidazo[1,2-a]pyrazine.png
5-chloroimidazo[1,2-a]pyrazine.png