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Bioorg Med Chem Lett. 2009 Apr 1;19(7):1879-82. doi: 10.1016/j.bmcl.2009.02.069. Epub 2009 Feb 21.

Syntheses of novel 2,3-diaryl-substituted 5-cyano-4-azaindoles exhibiting c-Met inhibition activity.

Author information

1
Clemens-Schöpf Institute of Organic Chemistry and Biochemistry, Technical University of Darmstadt, Petersenstrasse 22, 64287 Darmstadt, Germany. hannes.koolman@merck.de

Abstract

Herein we report the syntheses of 2,3-diaryl-substituted pyrrolo[3,2-b]pyridine-5-carbonitriles via a one-pot 5-endo-dig-cyclization/protection reaction followed by palladium catalyzed arylation. In addition, a complementary synthesis route employing Larock methodology is applied to efficiently explore further aryl moieties in the 2-position. The novel compounds' expedient c-Met receptor tyrosine kinase inhibition activity is discussed.

PMID:
19269177
DOI:
10.1016/j.bmcl.2009.02.069
[Indexed for MEDLINE]

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