Synthesis,Configuration Judgment and Potentiation Activity of (2S,3S,E)-4-(3,4-Dihydroxybenzylidene)-3-(3,4-dihydroxyphenyl)-5-oxotetrahydrofuran-2-carboxylic Acid

被引：0

作者：

张骏良 ^{[1
]}

吕志良 ^{[2
]}

钟家亮 ^{[3
]}

陈代杰 ^{[1
]}

李默影 ^{[1
]}

张建斌 ^{[1
]}

机构：

[1] State Key Laboratory of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry

[2] Zhangjiang Branch Institute of China State Institute of Pharmaceutical Industry

[3] Shanghai Institute of Pharmaceutical Industry

来源：

结构化学 | 2017年 / 36卷 / 09期

关键词：

total synthesis; crystal structure; potentiation activity; traditional Chinese medicine;

D O I：

暂无

中图分类号：

O626 [杂环化合物]; TQ460.1 [基础理论];

学科分类号：

070303 ; 081704 ; 1007 ;

摘要：

The title compound（2S,3S,E）-4-（3,4-dihydroxybenzylidene）-3-（3,4-dihydroxyphenyl）-5-oxotetrahydrofuran-2-carboxylic acid was synthesized and the 2D structure was characterized by;H-NMR;C-NMR and LCMS. The absolute configuration was determined by single-crystal X-ray diffraction of the key intermediate（2S,3S,E）-ethyl 4-（3,4-dimethoxybenzylidene）-3-（3,4-dimethoxyphenyl）-5-oxotetrahydrofuran-2-carboxylate. The crystal belongs to tetragonal system, space group P4;with a = 13.0665（2）, b = 13.0665（2）, c = 13.4735（2） ?, V = 2300.4（6） ?;, Z = 4, D;= 1.278 g/cm;, μ（CuKα） = 0.801 mm;, F（000） = 936, S = 1.050, R = 0.0364 and wR(I > 2σ（I）) = 0.1071. X-ray diffraction results showed that the molecular structure is stabilized totally by Van der Waals force. The antibacterial activity tests showed that the title compound possesses slight synergistic effect against MRSA and Acinetobacter baumanii.

引用

页码：1418 / 1424

页数：7

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