Visible light-induced cascade <i>N</i>-alkylation/amidation reaction of quinazolin-4(3<i>H</i>)-ones and related N-heterocycles
作者:Jiexiong Mai、Ziwei Huang、Shaohuan Lv、Quan Chen、Rongrong Chen、Feng Xie、Jun Wang、Bin Li
DOI:10.1039/d2ob02226e
日期:——
An efficient and visible light-promoted cascade N-alkylation/amidation of quinazolin-4(3H)-ones with benzyl halides and allyl halides has been described for the first time to provide a convenient access to quinazoline-2,4(1H,3H)-diones. This cascade N-alkylation/amidation reaction shows good functional group tolerance and could also be applied to N-heterocycles such as benzo[d]thiazoles, benzo[d]imidazoles
首次描述了喹唑啉-4(3 H )-与苄基卤化物和烯丙基卤化物的有效且可见光促进的级联N-烷基化/酰胺化,以提供对喹唑啉-2,4(1 H)的便捷途径,3 H )-二酮。这种级联N-烷基化/酰胺化反应显示出良好的官能团耐受性,也可应用于 N-杂环,如苯并 [ d ] 噻唑、苯并 [ d ] 咪唑和喹唑啉。对照实验表明,K 2 CO 3在这种转化中起着重要作用。
HEDAYATULLAH M., C. R. ACAD. SCI., 1979, C 289, NO 14, 365-367
作者:HEDAYATULLAH M.
DOI:——
日期:——
SUBSTRATE-MIMETIC AKT INHIBITOR
申请人:Sebti Said M.
公开号:US20100009397A1
公开(公告)日:2010-01-14
Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.
US8822524B2
申请人:——
公开号:US8822524B2
公开(公告)日:2014-09-02
Hedayatullah, Mir, Journal of Heterocyclic Chemistry, 1981, vol. 18, p. 339 - 342