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Synfacts 2008(1): 0008-0008  
DOI: 10.1055/s-2007-991494
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of the PKCβ Inhibitor JTT-010

Contributor(s): Philip Kocienski
M. Tanaka, M. Ubukata, T. Matsuo, K. Yasue, K. Matsumoto, Y. Kajimoto, T. Ogo, T. Inaba*
Japan Tobacco Inc., Osaka, Japan
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Publication History

Publication Date:
18 December 2007 (online)

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Significance

A new approach to the construction of the 2,3-dihydro-1H-pyrrolo[1,2-a]indole ring system D begins with nucleophilic cleavage of an activated cyclopropane ring B followed by an intramolecular addition-elimination reaction. The reaction sequence enabled abbreviation of a synthesis of JTT-010, a promising selective protein kinase C-β inhibitor.