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

…, DJ Post-Munson, JT Trojnacki, K Yeleswaram…

文献索引：Hewawasam, Piyasena; Gribkoff, Valentin K.; Pendri, Yadagiri; Dworetzky, Steven I.; Meanwell, Nicholas A.; Martinez, Eduardo; Boissard, Christopher G.; Post-Munson, Debra J.; Trojnacki, Joanne T.; Yeleswaram, Krishnaswamy; Pajor, Lorraine M.; Knipe, Jay; Gao, Qi; Perrone, Robert; Starrett Jr., John E. Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 7 p. 1023 - 1026

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被引用次数: 103

摘要

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.