32418-03-4Relevant articles and documents
Effective C5-Arylation of Peptide-Integrated Oxazoles: Almazole D
Oberheide, Ansgar,Arndt, Hans-Dieter
supporting information, p. 1132 - 1136 (2020/12/22)
An efficient functionalization approach of oxazoles by using Pd-catalyzed cross-coupling reactions is reported. Oxazolone formation and subsequent sulfamoylation in situ are facilitated by employing N,N-diethylsulfamoyl imidazolium triflate. Cross-couplings provide both oxazole-arenes and oxazole-heteroarenes and were compatible with sensitive and epimerization-prone substrates, as exemplified by the total synthesis of the natural product almazole D. (Figure presented.).
Structure-activity relationships of heteroaromatic esters as human rhinovirus 3C protease inhibitors
Im, Isak,Lee, Eui Seung,Choi, Soo Jeong,Lee, Ju-Yeon,Kim, Yong-Chul
scheme or table, p. 3632 - 3636 (2010/03/24)
Human rhinovirus 3C protease (HRV 3Cpro) is known to be a promising target for development of therapeutic agents against the common cold because of the importance of the protease in viral replication as well as its expression in a large number of serotypes. To explore non-peptidic inhibitors of HRV 3Cpro, a series of novel heteroaromatic esters was synthesized and evaluated for inhibitory activity against HRV 3Cpro, to determine the structure-activity relationships. The most potent inhibitor, 7, with a 5-bromopyridinyl group, had an IC50 value of 80 nM. In addition, the binding mode of a novel analog, 19, with the 4-hydroxyquinolinone moiety, was explored by molecular docking, suggesting a new interaction in the S1 pocket.
Cycloadditions of Isocyanides to Azomethine Ylides. Synthesis and Properties of 1-Phthalimidoazetidines
Charrier, Josiane,Foucaud, Andre',Person, Herve',Loukakou, Emile
, p. 481 - 486 (2007/10/02)
Reactions of isocyanides with 1-phthalimidoaziridines 1,5, and 11 gave 1-phthalimidoazetidines by cycloaddition to the azomethine ylides that are in equilibrium with the aziridines. (tert-Butylimino)azetidines and (tert-octylimino)azetidines rearranged into open-chain azadienes.Reactions of hydrazine hydrate with 1-phthalimidoazetidines did not give the corresponding N-aminoazetidines, but rather their decomposition products, nitrogen and enamino esters.