Friday, February 12, 2010

Sharpless patent claims and click chemistry











This patent by Sharpless et al was issued on May 20, 2008, titled "Copper-catalysed ligation of azides and acetylenes ". It claims:

1. A Cu(I) catalyzed process for preparing a 1,4-disubstituted 1,2,3-triazole comprising: contacting an organic azide and a terminal alkyne with a catalytic quantity of Cu(I) ion for a time sufficient to form by cycloaddition a 1,4-disubstituted 1,2,3-triazole.
2. The process in accordance with claim 1 wherein the cycloaddition is carried out at ambient temperature.
3. The process in accordance with claim 1 wherein equimolar amounts of the organic azide and the terminal alkyne are contacted with a catalytic quantity of the Cu(I) ion.
4. The process in accordance with claim 1 wherein said catalytic quantity of the Cu(I) ion is generated in situ by reduction of Cu(II) to Cu(I) with a reducing agent.
5. The process in accordance with claim 4 wherein the reducing agent is sodium ascorbate.
6. The process in accordance with claim 4 wherein Cu(II) sulfate pentahydrate is reduced by sodium ascorbate.

It appears the claim is the Cu(+) catalysed reaction ITSELF. Already having some impact on biotechnology and materials science, evidenced by licensing and product launches, it is expected to have a larger influence on more industries such as medicinal chemistry, nanotechnology, biomedical science, etc.

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