873426-76-7Relevant articles and documents
Copper-Photocatalyzed Borylation of Organic Halides under Batch and Continuous-Flow Conditions
Nitelet, Antoine,Thevenet, Damien,Schiavi, Bruno,Hardouin, Christophe,Fournier, Jean,Tamion, Rodolphe,Pannecoucke, Xavier,Jubault, Philippe,Poisson, Thomas
supporting information, p. 3262 - 3266 (2019/02/13)
The copper-photocatalyzed borylation of aryl, heteroaryl, vinyl and alkyl halides (I and Br) was reported. The reaction proceeded using a new heteroleptic Cu complex under irradiation with blue LEDs, giving the corresponding boronic-acid esters in good to excellent yields. The reaction was extended to continuous-flow conditions to allow an easy scale-up. The mechanism of the reaction was studied and a mechanism based on a reductive quenching (CuI/CuI*/Cu0) was suggested.
SUBSTITUTED METHYL PYRAZOLOPYRIMIDINONE AND METHYL IMIDAZOPYRAZINONE COMPOUNDS AS PDE1 INHIBITORS
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Paragraph 064, (2019/06/20)
A chemical entity of Formula (I) or Formula (II): wherein Ra, Rb, Re, and Rf have any of the values described herein, and compositions comprising such chemical entities; methods of making them; and their use in
Base-Free Palladium-Catalyzed Borylation of Aryl Chlorides with Diborons
Yamamoto, Yutaro,Matsubara, Hiroshi,Yorimitsu, Hideki,Osuka, Atsuhiro
, p. 2317 - 2320 (2016/07/28)
The base-free palladium-catalyzed borylation of aryl chlorides with diborons was achieved. The base-free conditions offered acceptable functional group compatibility. Based on experimental and computational studies, it was shown that smooth boryl transfer from the diborons to the arylpalladium chloride was promoted by strong interaction between the Lewis acidic boron and the chlorine atom on palladium.
Ni/Cu-Catalyzed Defluoroborylation of Fluoroarenes for Diverse C-F Bond Functionalizations
Niwa, Takashi,Ochiai, Hidenori,Watanabe, Yasuyoshi,Hosoya, Takamitsu
supporting information, p. 14313 - 14318 (2015/11/27)
Ni/Cu-catalyzed transformation of fluoroarenes to arylboronic acid pinacol esters via C-F bond cleavage has been achieved. Further versatile derivatization of an arylboronic ester has allowed for the facile two-step conversion of a fluoroarene to diverse functionalized arenes, demonstrating the synthetic utility of the method.
Total synthesis of eryvarin H and its derivatives and their biological activity as ERRγ inverse agonist
Koo, Ja Young,Oh, Sangmi,Cho, Seung-Rye,Koh, Minseob,Oh, Won-Keun,Choi, Hueng-Sik,Park, Seung Bum
supporting information, p. 5782 - 5786 (2013/09/12)
Total synthesis of eryvarin H and a biological investigation of its analogues as a potential inverse agonist of ERRγ are described here. Among the 13 analogues prepared by the modular synthetic route, eryvarin H and compound 12 showed meaningful ERRγ inverse agonistic activities along with moderate selectivity over ERα and other nuclear receptors in the cell-based reporter gene assay.
Addition of arylboronic acids to arylpropargyl alcohols en route to indenes and quinolines
Panteleev, Jane,Huang, Richard Y.,Lui, Erica K. J.,Lautens, Mark
, p. 5314 - 5317 (2011/12/01)
A regio- and stereoselective rhodium-catalyzed synthesis of trisubstituted allylic alcohols is described. The utility of these synthons is demonstrated in a convenient synthesis of indenes and quinolines.
