Good news to malaria suffering countries

I just read a very nice peace of work regarding malaria-treatment. This inspires me to show three very nice publications to you, which I discovered in the last feew weeks.  Three of them are very impressive papers, the scientific results could give malaria treatment a push. As it is not longer a secret that malaria resistance against artemisinin was discovered at the cambodian border, it is very important to elaborate new affordable drugs or to improve old ones.

But as you can read in these articles (or at least in the abstracts) there are three promising things in the pipeline.

Article one:
Malaria-infeted mice are completely cured

It describes that mice can be cured completely by artemisinin-based derivatives, the so called anilides, in combination with mefloquine. Anilides still bear a trioxane unit which is the active group in artemisinin but are further decorated with some sulfur-containing groups. These derivatives can easily be obtained by simple chemical manipulations of dihydroartemisinin and show remarkable activity against Plasmodium berghei.

Article two:
Production of the antimalarial drug precursor artemisinic acid in engineered yeast

This very interesting and trendsetting paper describes the production of artemisinic acid in genetically changed yeast. By that you can develope a very efficient way to provide infected people with artemisinin. It is just neccessary to further modify the obtained compound by two oxidation steps to get the desired antimalarial agent.

You could have asked now….ok, there is a cheap and efficient way to produce artemisinic acid and the two steps to yield artemisinin out of this acid are very straightforward as well. But why there is no application to supply people with this drug? Especially if you consider that the price for natural artemisinin fluctuates heavily as it depends on good harvests of the plant Artemisia annua.  Listen up, here comes the answer!

Article three:
Continuous-flow synthesis of the anti-malaria drug artemisinin

Seeberger and colleagues reported about a very efficient way to achieve the last synthetic steps in large scale reactions. They are using a selfbuilt flow-reactor to manage this conversions and end up with a good yield of this important drug. They claym that it is possible to produce 200g of artemisinin within one day and 1500 reactors would be enough to cover the global need for this drug. I really think that this is a promissing technique to produce affordable artemisinin-based therapeutics. But this achivement is just successful if the people do not longer stick to artemisinin monotherapies as this enforces the resistance of plasmodium towards this drug.

Stay tuned 😉

Kaeptn Future

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LC-MS check, column chromatography, HRMS check

Today I did it!

The hydrolysis of a very stable diethyl-acetal with 2M hydrogenchloride worked (THF, 2 h, reflux) and the following intramolecular cyclisation of a beta-ketoamide with the now deprotected aldehyde worked as well. LC-MS reactioncontroll is a really helpfull tool to get quick information about a conversion. I proceeded to check wether the compund is TLC stable or not by simple 2D-TLC. Yes! It is! Quickly ran a column with HRMS-analysis of the collected Spot. Perfect! It´s a mixture of three compounds with nearly the same Rf-value ! The cyclised compound, the cyclised compound including elimination of the newly formed alcohol and traces of my final compound! Tomorrow I will give sodiumhydroxide another chance to give me the cyclised and eliminated compound.  Then it is just one step away from the total synthesis of…..

I just want you to participate in this progress and I want to show, how emotional chemistry can be. More details regarding the synthesis strategy and the final product will follow as soon as possible.

 

Stay tuned 😉

KaeptnFuture

This dude is so awesome

I am really proud of a very very young guy….his name is Philip Köster, he is 17 years old and lives on Grand Canaria. What else should one do on this tiny, boring(?) island than using the wind and the waves to have some fun with a board under your feet?!? And if you can make this on a professional level, you will soon call attention to your carreer. As it just happend to this young guy. He is now sponsored by the major carmaker „Volkswagen“ Read the article. And if you ask me, he really deserves it because although he is very successful and is becoming more and more popular, he still is  a down-to-earth, nice person without airs and graces. That´s how I got to know him last saturday at the fair „Boot 2012“ in Düsseldorf.

I am pretty sure he will do as I told him „Lass Dir diese Saison nicht die Butter vom Brot nehmen!“

Phlip Köster, Boot 2012

Stay tuned 😉

Kaeptn Future

Let´s switch….

….to english! I just recognized that switching to english has two major advantages….first of all the majority of wordpress users seem to use the english language….secondary…I can improve my english! Isn´t that fantastic? Let´s just do it and if you recognise any mistakes, don´t hesitate to contact me 😉

Stay tuned 😉

Kaeptn Future