Syntheses of novel 2,3-diaryl-substituted 5-cyano-4-azaindoles exhibiting c-Met inhibition activity
摘要:
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. (C) 2009 Elsevier Ltd. All rights reserved.
Compounds of the formula (I), in which X
1
, X
2
, X
3
, X
4
, R
1
, R
2
, R
3
and R
4
have the meanings indicated in Claim
1
, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumours.
Verbindungen der Formel (I) worin X1, X2, X3, X4, R1, R2, R3 und R4 die in Anspruch 1 angegebenen Bedeutungen haben, sind Inhibitoren der Tyrosinkinasen, insbesondere der Met-Kinase und können u.a. zur Behandlung von Tumoren eingesetzt werden.