77335-93-4Relevant academic research and scientific papers
ZnCl2-Catalyzed [3 + 2] Cycloaddition of Benzimidates and 2 H-Azirines for the Synthesis of Imidazoles
Shi, Shoujie,Xu, Kang,Jiang, Cheng,Ding, Zhenhua
, p. 14791 - 14796 (2018/11/23)
ZnCl2-catalyzed [3 + 2] cycloaddition reaction of benzimidates and 2H-azirines has been developed. This convenient method allowed the efficient construction of a series of multisubstituted imidazoles in moderate to good yields under mild reaction conditions. This transformation exhibits good reactivity and high functional group tolerance.
Synthesis of di- and tri-substituted imidazole-4-carboxylates via PBu3-mediated [3+2] cycloaddition
Hsu, Mei-Yuan,Dietrich, Justin,Hulme, Christopher,Shaw, Arthur Y.
, p. 1538 - 1542 (2013/05/21)
Some new di- and trisubstituted imidazole-4-carboxylates were prepared from amidoacetic acids 3 in the present report. The key step to establish such imidazole- 4-carboxylates stemmed from the PBu3-mediated [3+2] cycloaddition between in situ-generated Δ2-oxazolinone 4 and ethyl cyanoformate6. Our results indicated that trisubstituted imidazoles 7-20 were afforded in better yields than those of disubstituted imidazoles 21-27. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications1 to view the free supplemental file. Copyright Taylor & Francis Group, LLC.
AROMATIC HETEROCYCLIC DERIVATIVE HAVING TRPV4-INHIBITING ACTIVITY
-
Page/Page column 84, (2012/11/07)
A compound having TRPV4 inhibitory activity or a pharmaceutically acceptable salt thereof is provided. The present invention is related to a compound represented by the formula (I). wherein R1a is substituted or unsubstituted alkyl or the like;
Discovery of cell-active phenyl-imidazole Pin1 inhibitors by structure-guided fragment evolution
Potter, Andrew,Oldfield, Victoria,Nunns, Claire,Fromont, Christophe,Ray, Stuart,Northfield, Christopher J.,Bryant, Christopher J.,Scrace, Simon F.,Robinson, David,Matossova, Natalia,Baker, Lisa,Dokurno, Pawel,Surgenor, Allan E.,Davis, Ben,Richardson, Christine M.,Murray, James B.,Moore, Jonathan D.
scheme or table, p. 6483 - 6488 (2010/12/18)
Pin1 is an emerging oncology target strongly implicated in Ras and ErbB2-mediated tumourigenesis. Pin1 isomerizes bonds linking phospho-serine/threonine moieties to proline enabling it to play a key role in proline-directed kinase signalling. Here we report a novel series of Pin1 inhibitors based on a phenyl imidazole acid core that contains sub-μM inhibitors. Compounds have been identified that block prostate cancer cell growth under conditions where Pin1 is essential.
Syntheses of 2-Arylimidazole Derivatives through Annelations Employing Benzylamines
Veronese, A.C.,Cavicchioni, G.,Servadio, G.,Vecchiati, G.
, p. 1723 - 1725 (2007/10/02)
Annelations of benzylamines with hydroximino derivatives of pentane-2,4-dione or of alkyl acetoacetates, acetoacetamides, and acetoacetanilides, afford imidazole derivatives and provide easy incorporation of the benzylic carbon and nitrogen in the heterocycle.The limits of the reaction have been explored.
