Macrocyclic bisindolylmaleimides: synthesis by inter-and intramolecular alkylation

…, LL Winneroski, CA Krumrich, KA Sullivan…

文献索引：Faul, Margaret M.; Winneroski, Leonard L.; Krumrich, Christine A.; Sullivan, Kevin A.; Gillig, James R.; Neel, David A.; Rito, Christopher J.; Jirousek, Michael R. Journal of Organic Chemistry, 1998 , vol. 63, # 6 p. 1961 - 1973

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被引用次数: 35

摘要

Macrocyclic bisindolylmaleimides 1-4 have been identified as competitive reversible inhibitors of PKC β1 and β2 and are being advanced to the clinic for evaluation as a treatment of retinopathy associated with diabetic complications. Highly convergent and stereoselective syntheses of 1-4 have been developed. The key synthetic step involves intermolecular alkylation of symmetrical bisindolylmaleimide 9 with chiral bisalkylating ...