3134-35-8Relevant academic research and scientific papers
Synthesis of Bis-heteroaryls Using Grignard Reagents and Pyridylsulfonium Salts
Horan, Alexandra M.,Duong, Vincent K.,McGarrigle, Eoghan M.
, p. 9089 - 9093 (2021/11/30)
Herein are reported ligand-coupling reactions of Grignard reagents with pyridylsulfonium salts. The method has wide functional group tolerance and enables the formation of bis-heterocycle linkages, including 2,4′-, 2,3′-, and 2,2′-bipyridines, as well as pyridines linked to pyrimidines, pyrazines, isoxazoles, and benzothiophenes. The methodology was successfully applied to the synthesis of the natural products caerulomycin A and E.
Nucleophilic C-H Etherification of Heteroarenes Enabled by Base-Catalyzed Halogen Transfer
Puleo, Thomas R.,Klaus, Danielle R.,Bandar, Jeffrey S.
supporting information, p. 12480 - 12486 (2021/08/24)
We report a general protocol for the direct C-H etherification of N-heteroarenes. Potassium tert-butoxide catalyzes halogen transfer from 2-halothiophenes to N-heteroarenes to form N-heteroaryl halide intermediates that undergo tandem base-promoted alcohol substitution. Thus, the simple inclusion of inexpensive 2-halothiophenes enables regioselective oxidative coupling of alcohols with 1,3-azoles, pyridines, diazines, and polyazines under basic reaction conditions.
AZACARBOLINE DERIVATIVES, PREPARATION METHOD THEREOF AND THERAPEUTIC USE OF SAME
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Page/Page column 22, (2011/08/04)
The invention relates to novel azacarbonlines having formula (I), wherein: R3, R4 represent independently H; hal; CF3; substituted oxy, optionally substituted alkoxy; optionally substituted amino; substituted carbonyl; optionally substituted carboxyl; optionally substituted amide; sulphur, such as optionally substituted sulphones, sulphoxides or sulphides; linear, branched or cyclic C1-C10 alkyl optionally comprising an optionally substituted heteroatom; optionally substituted linear, branched or cyclic C2-C7 alkenyl; optionally substituted linear or branched C2-C6 alkynyl; optionally substituted aryl or heteroaryl; of which may be optionally substituted; in the form of a base or an acid addition salt. The invention also relates to the use of same in therapeutics for the treatment of cancer and to synthesis methods.
Some regioselective cross-coupling reactions of halopyridines and halopyrimidines
Simkovsky, Nadja M.,Ermann, Monika,Roberts, Stanley M.,Parry, David M.,Baxter, Andy D.
, p. 1847 - 1849 (2007/10/03)
A high yielding approach for the synthesis of bipyridines, pyridylpyrimidines and pyridylquinolines was described. The approach employed regioselective cross-coupling reactions using palladium catalysts. The synthesis involved lithiation of a heterocycle at low temperatures, and eliminated the need to prepare and handle active zinc. The bipyridine group in the compounds exhibits antibiotic and cytotoxic properties and some have potential to be used as fungicides.
