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Cereprotec Inc. and Institute of Applied Chemistry at Hebrew University are working together to synthesise new Glycoluril Derivatives with Possible Neuroprotection Effects.
According to report of Institute of Applied Chemistry they have performed the third step as it appears in the synthesis route scheme. This took much longer than the other steps, after all, this reaction doesn't appear in any literature and in the end only took two and half weeks. This research is fully sponsored by Cereprotec Incorporated www.cereprotec.com a US company that already runs clinical tests of their first drug Cereprotex .
In the reaction between compound II and III, one gets two main products, three additional compounds in small quantities plus unreacted starting materials and one main side product. All together there were 8 compounds in the reaction mixture.
One of the main materials precipitated out from the mixture and was removed via filtration from the reaction mixture. This material was cleaned up via crystallization but turned out not to be the desired compound.
The second main material was separated via silica gel column chromatography. Unfortunately, this main material came off at the same Rf value as another material. They tested out several solvents and found that ethyl acetate was able to crystallize out the main material.
Using NMR and elemental analysis, Institute of Applied Chemistry were able to prove that the crystallized out material is indeed Compound III. Yield was 17%. Two grams of material was obtained, enough to try out Stage IV.
This step can be repeated in the future in order to produce more of compound III.
Page Updated: 8/17/2008 10:40:58 AM