- Synthesis of 3-Halo-7-azaindoles through a 5- endo -dig Electrophilic Cyclization Reaction
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Biologically useful 7-azaindoles were synthesized by electrophilic cyclization of 3-alkynyl- N, N -dimethylpyridine-2-amines with molecular iodine. By this simple atom-economical approach under ambient reaction conditions, a library of interesting 3-iodo-7-azaindoles were synthesized in high yields. To synthesize the corresponding 3-bromo- and 3-chloro-7-azaindoles, an environmentally benign copper-mediated cyclization was employed, with inexpensive, nontoxic, and noncorrosive sodium chloride and sodium bromide as the sources of chlorine and bromine, respectively.
- Cunningham, Christopher,Kesharwani, Tanay,Naran, Kajal,Philips, Aimee
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supporting information
p. 1246 - 1252
(2019/06/08)
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- One-Pot Coupling-Cyclization-Alkylation Synthesis of 1,2,5-Trisubstituted 7-Azaindoles in a Consecutive Three-component Fashion
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1,2,5-Trisubstituted 7-azaindoles are rapidly and efficiently prepared in a one-pot, copper-free alkynylation-cyclization-alkylation sequence starting from unprotected 2-aminopyridyl halides in a consecutive three-component fashion. By extension to a consecutive four-component coupling-cyclization-iodination-alkylation synthesis of 3-iodo-1-methyl-2-phenyl-1 H -pyrrolo[2,3- b ]pyridine, a concise synthesis of SIS3, a selective TGF-β1 and signaling inhibitor, was realized.
- Lessing, Timo,Müller, Thomas J. J.
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supporting information
p. 1743 - 1747
(2017/10/06)
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- BICYCLIC HETEROARYL DERIVATIVES AS KINASE INHIBITORS
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The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula 1: wherein Het, X, R1 and R2 are as defined herein.
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Paragraph 00488
(2013/06/06)
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- 2-SUBSTITUTED AZAIN DOLES AND 2 SUBSTITUTED THIENOPYRROLES, THEIR PRECURSORS AND NOVEL PROCESSES FOR THE PREPARATION THEREOF
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The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, an
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Page/Page column 144
(2010/11/30)
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- A general modular method of azaindole and thienopyrrole synthesis via Pd-catalyzed tandem couplings of gem-dichloroolefins
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(Chemical Equation Presented) A palladium-catalyzed reaction of gem-dichloroolefins and a boronic acid via a tandem intramolecular C-N and intermolecular Suzuki coupling process gave corresponding substituted azaindoles or thienopyrroles. This method is a
- Fang, Yuan-Qing,Yuen, Josephine,Lautens, Mark
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p. 5152 - 5160
(2008/02/07)
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