Synthesis of Pyrrolopyridines (Azaindoles) | Request PDF

PCT Patent Application (2002), WO 0208224 A1 and more than 34 2-carboxy esters of such azaindoles with varioussubstitution are found in Scifinder.

The synthesis of 1H-Pyrrolo[2,3-b]pyridine-4-carboxylic acid, methyl ester has been described in the literature by Allegretti et.

Facile Synthesis of 2‐Substituted 4‐Azaindoles: …

Syntheses of novel 2,3-diaryl-substituted 5-cyano-4-azaindoles exhibiting ..
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Transition metal catalyzed synthesis of 5-azaindoles

The methods used to prepare compounds of Formula I from the heterocyclic carboxylates are those described for Schemes 1, 1A and 2.

Schemes I-1 through I-12 depict methods and conditions for the synthesis of azaindole and indole carboxylates according to the first strategy wherein an indole or azainole containing a carboxylate moiety is synthesized.

Synthesis of 4-(cyclic dialkylamino)-7-azaindoles by ..

Tropomyosin-related kinase A (TrkA) is considered a promising target in the development of a therapeutic treatment of cancer and pain. In this study, we designed and synthesized a series of novel 7-azaindole-based Trk kinase inhibitors through the structure-based design strategy. By varying the functional groups at the 3 and 5 positions of a 7-azaindole scaffold, we studied the structure–activity relationships (SAR) profiles and identified a series of potent Trk inhibitors. Representative derivatives showed desirable activity in cellular proliferation and apoptosis assays. Moreover, these inhibitors exhibited noteworthy antiangiogenic activity.

Synthesis of pyrrolopyridines (Azaindoles ..
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8 these pyrrolopyridines are ..

Azaindoles (4) find widespread use in drug discovery yet methods which permit access to all possible regioisomers are limited and their purchase is costly.1,2 Whelligan previously published a two-step synthesis of all regioisomers from chloro- or bromo-aminoarenes which involves Suzuki coupling with ethoxyvinylborolane 2, to give an ethoxyvinylarene 3, followed by acid-mediated cyclisation.3 We are now investigating the versatility of the ethoxyvinylarenes 3 in terms of producing substituted azaindoles or tricycles in one step.

Recent advances of pyrrolopyridines ..

This published application describes methodology for functionalizing azaindoles which is hereby incorporated as available and instructive to someone skilled in the art.

The synthesis of 1H-Pyrrolo[2,3-b]pyridine-2-carboxylic acid, methyl ester has been described in the literature by Davies et.

13/06/2014 · The methods of synthesis of 2 ..