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Synthesis 1995; 1995(12): 1511-1516
DOI: 10.1055/s-1995-4146
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A General Approach to the Synthesis of Bisindolylmaleimides: Synthesis of Staurosporine Aglycone

Margaret M. Faul* , Kevin A. Sullivan, Leonard L. Winneroski
  • *Chemical Process Research & Development, Eli Lilly & Company, Indianapolis, Indiana 46285-4813, USA, Fax +1(317)2764507
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Publikationsdatum:
31. Dezember 2000 (online)

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Bisindolylmaleimides are prepared in 65-95% yield by reaction of an indole Grignard with either 2,3-dichloro-N-methylmaleimide or 2,3-dichloromaleimide. A one-step synthesis of arcyriarubin A in 72% yield affords ready access to the staurosporine aglycone.

dihalomaleimides - indolyl-MgBr - bisindolylmaleimides - arcyriarubin A - staurosporine aglycone

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