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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 
 
 
 
 

The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels.

3-Aryl-3-fluorooxindoles can be efficiently synthesized in two steps by the addition of an aryl Grignard to an isatin, followed by treatment with DAST. Oxindole 1 (BMS-204352; MaxiPost) can be isolated using chiral HPLC or prepared by employing chiral resolution. Cloned maxi-K channels are opened by 1, which demonstrates a brain/plasma ratio >9 in rats.[1]

References

  1. The synthesis and characterization of BMS-204352 (MaxiPost) and related 3-fluorooxindoles as openers of maxi-K potassium channels. Hewawasam, P., Gribkoff, V.K., Pendri, Y., Dworetzky, S.I., Meanwell, N.A., Martinez, E., Boissard, C.G., Post-Munson, D.J., Trojnacki, J.T., Yeleswaram, K., Pajor, L.M., Knipe, J., Gao, Q., Perrone, R., Starrett, J.E. Bioorg. Med. Chem. Lett. (2002) [Pubmed]
 
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