具有咖啡酰基和没食子酰基的β-二酮酸及喹噁啉酮类HIV整合酶抑制剂的设计合成及其对Cu2+的选择性识别

An efficient procedure for the synthesis of caffeoyl-and galloyl-containing β-diketoacid derivatives linked byarylamide was reported by,in the key step,dissolving the corresponding phenyl methyl ketone in THF/DME in thepresence of NaOMe as base and dimethyl oxalate as oxalylation reagent,and then separating the sodium ketoe-nolate ester.The resulting β-diketoacids underwent further condensation reaction with o-phenylenediamine to gen-erate quinoxalone derivatives in good yield,rather than 2-benzimidazol.The preliminary ion binding properties ofquinoxalone derivatives were also investigated.UV-Vis spectra showed that these compounds could selectively rec-ognize Cu~(2 )ion in ethanol and form a 1∶2 complex.

Design,Synthesis and Cu2+ Recognition of β‐Diketoacid and Quinoxalone Derivatives Bearing Caffeoyl or Galloyl Moieties Linked by Arylamide as Potential HIV Integrase Inhibitors

An efficient procedure for the synthesis of caffeoyl‐ and galloyl‐containing β‐diketoacid derivatives linked by arylamide was reported by, in the key step, dissolving the corresponding phenyl methyl ketone in THF/DME in the presence of NaOMe as base and dimethyl oxalate as oxalylation reagent, and then separating the sodium ketoenolate ester. The resulting β‐diketoacids underwent further condensation reaction with o‐phenylenediamine to generate quinoxalone derivatives in good yield, rather than 2‐benzimidazol. The preliminary ion binding properties of quinoxalone derivatives were also investigated. UV‐Vis spectra showed that these compounds could selectively recognize Cu²⁺ ion in ethanol and form a 1:2 complex.