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2010年01月27日

【期刊论文】Synthesis, Crystal Structure, and Insecticidal Activities of Highly Congested Hexahydroimidazo[1,2-a]pyridine Derivatives: Effect of Conformation on Activities†

李忠, XUSHENG SHAO, ZHIPING XU, XIANFENG ZHAO, XIAOYONG XU, * LIMING TAO, ZHONG LI, * AND XUHONG QIAN

J. Agric. Food Chem. XXXX, XXX, 000-000 A,-0001,():

-1年11月30日

摘要

A series of hexahydroimidazo[1,2-a]pyridine derivatives were designed and synthesized through aza-Diels-Alder reactions and evaluated for insecticidal activities. Compounds 6a-d with endoconformation were endowed with excellent insecticidal activities against cowpea aphid (Aphis craccivora) and armyworm (Pseudaletia separata Walker), whereas exo-compounds 7a-d showed only low activities against cowpea aphid. The difference in activities between the endo- and exoconformations indicated that conformation was the determinant of life or death of the insects for these compounds.

Diels-Alder reaction, insecticide, conformation, activities

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2010年01月27日

【期刊论文】Enantiocontrolled Synthesis of (-)-9-epi-Pentazocine and (-)-Aphanorphine

李忠, Xiaobao Yang, †, ‡ Hongbin Zhai, *, † and Zhong Li*, ‡

Org. Lett., Vol. 10, No.12, 2008,-0001,():

-1年11月30日

摘要

We have developed novel asymmetric routes to (-)-9-epi-pentazocine and (-)-aphanorphine from a D-tyrosine derivative. The tricyclic frameworks of (-)-9-epi-pentazocine and (-)-aphanorphine were assembled stereoselectively via intramolecular Friedel-Crafts reaction of the corresponding bicyclic precursors, generated with titanium-promoted enyne cyclization and indium-initiated atom-transfer radical cyclization, respectively.

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2010年01月27日

【期刊论文】1,3,4-Oxadiazole-3(2H)-carboxamide derivatives as potential novel class of monoamine oxidase (MAO) inhibitors: Synthesis, evaluation, and role of urea moiety

李忠, Shaoyong Ke, Zhong Li, Xuhong Qian *

Bioorganic & Medicinal Chemistry 16(2008)7565-7572,-0001,():

-1年11月30日

摘要

A new series of 1,3,4-oxadiazole-3(2H)-carboxamide derivatives have been synthesized by direct heterocyclization reaction of substituted benzoylisocyanate with various aroylhydrazones as novel monoamine oxidase inhibitors (MAOIs). The target molecules have been identified on the basis of satisfactory analytical and spectra (IR, 1H NMR, 13C NMR, and HR-MS) data. The newly synthesized compounds were evaluated for their MAO inhibitory activity by kynuramine fluorimetric assay method. The preliminary results showed that most of the compounds have moderate inhibitory activities toward MAO at the concentration of 10-5-10-3 M. This work may provide a novel class of lead compounds with potential MAO inhibitions for further optimization.

1,, 3,, 4-Oxadiazole-3(, 2H), -carboxamide Heterocycle MAO inhibitor Urea

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2010年01月27日

【期刊论文】Chromogenic and fluorescent chemodosimeter for fluoride ion based on novel anion-catalyzed intramolecular hydrogen transferwz

李忠, Chuanxiang Liu, Xuhong Qian, * Guangqiang Sun, Liwei Zhao and Zhong Li*

New J. Chem., 2008, 32, 472-476,-0001,():

-1年11月30日

摘要

We have developed a chromogenic and fluorescent chemodosimeter 3, based on a novel anioncatalyzed intramolecular hydrogen transfer, which displayed drastic changes in UV-Vis absorption as well as fluorescence emission intensities showing selectively for F- over other anions.

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2010年01月27日

【期刊论文】Anion recognition by a novel Fipronil-based receptor: efficient deprotonation or stable intermolecular hydrogen bonding

李忠, Chuanxiang Liu, Xuhong Qian *, Jiaobing Wang, Zhong Li *

Tetrahedron Letters 49(2008)1087-1090,-0001,():

-1年11月30日

摘要

Strong electron-deficient heterocycles of acetyl Fipronil (F3) was designed and synthesized, its ability for anion recognition was investigated by UV and NMR analyses. This novel Fipronil-based receptor F3 shows strong binding affinity with acetate (P107 M1), phosphate or fluoride ion through efficient deprotonation. In addition, its interaction with chloride anion or other weak base anions through stable intermolecular H-bonding was also reported.

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  • 李忠 邀请

    华东理工大学,上海

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