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中国化学会第十四届全国有机合成化学学术研讨会

作者： Zhongxiang Zhu Qinghe Wang dulin kong Mingshu Wu Key Laboratory of Tropical Medicinal Plant Chemistry of the Ministry of Education College of Chemistry & Chemical EngineeringHainan Normal University

Many bicyclic polyhydropyrazolo[1,2-a]pyrazolone derivatives have important medicinal *** shown in Figure 1,compounds A and B are antibacterial agents that are analogues of penicillin and *** addition,nitrogen-containing bisphosphonate(N-BPs)drugs are used to treat a variety of bone resorption diseases,such as osteoporosis,Paget’s disease,and hypercalcemia due to *** are thought to act by inhibiting the enzyme farnesyl diphosphate synthase,resulting in inhibition of protein prenylation in *** is worth mentioning that most of the highly potent third-peneration BP drugs contain the nitrogen heterocyclic component in their molecular structures,as in risedronate and zoledronate,and for the treatment of bone diseases associated with excessive resorption,the cyclic nitrogen bisphosphonate(N-BPs)are up to 10,000-fold more active than the first-generation non-nitrogen containing BP,for example,***,the purposeful synthesis of new members of cyclic nitrogen containing N-BP family is of current interest for further development of more potent drugs.

关键词： azomethine imines vinylidene(bis)phosphonate cycloaddition

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An Efficient Catalyst-Free Multicomponent Synthesis Quinoline Derivatives via Friedel–Crafts Reaction in Water

An Efficient Catalyst-Free Multicomponent Synthesis Quinolin...

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中国化学会第十四届全国有机合成化学学术研讨会

作者： dulin kong Zhongxiang Zhu Qinghe Wang Qiang Lin Mingshu Wu Chemical Engineering College Nanjing University of Science and Technology School of Pharmaceutical Sciences Hainan Medical University Key Laboratory of Tropical Medicinal Plant Chemistry of the Ministry of Education College of Chemistry & Chemical Engineering Hainan Normal University

Quinoline derivatives have been widely used in the manufacture of dyes and the discovery of experimental drug candidates,and this scaffold has been found in numerous products with biological and pharmacological properties such as papaverine,camptothecine,XK469,R207910,Moxifloxacin and TMC 207.A variety of reactions *** reaction,Henry reaction and aldol reaction,Morita-Baylis Hillman reaction has been studied both‘in-water’and‘on-water’.However,the examples of catalyst free Friedel-Crafts reaction‘in-water’or‘on-water’are *** part of our continued interest in the synthesis of heterocyclic compounds and green chemistry,Along this line,we report a one pot condensation reaction of 1,3-dicarbonyl compounds,8-hydroxyquinoline and aromatic aldehydes under catalyst-free conditions via Friedel–Crafts reaction in water

关键词： quinoline water Friedel–Crafts reaction

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An Efficient and Clean Sulfenylation of Imidazoheterocycles with Sulfonyl Hydrazides in Water

An Efficient and Clean Sulfenylation of Imidazoheterocycles ...

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中国化学会·第十五届全国有机合成化学学术研讨会

作者： dulin kong Qinghe Wang Tiao Huang Qiang Lin Mingshu Wu Chemical Engineering College Nanjing University of Science and Technology School of Pharmaceutical Sciences Hainan Medical University Key Laboratory of Water Pollution Treatment&Resource Reuse of Hainan province College of chemistry and chemical engineering Hainan Normal University 南京理工大学

Imidazo[1,2-a]pyridines are recognized to exhibit a broad range of applications in pharmaceuticals and optoelectronics. Several commercially available drugs have the imidazo[1,2-a]pyridines motif in their core structure, for example, the sedative Zolpidem, the anxiolytic Alpidem or Saripidem, or the heart failure drug *** the past decades, significant efforts have been made for the construction of substituted imidazo[1,2-a]pyridine *** part of our continued interest in the synthesis of heterocyclic compounds and green chemistry, Herein we report the possible use of water as an efficient medium to introduce Sulfenylation of Imidazoheterocycles under ligand or additive free conditions at 120 ℃ under air(Fig.1).

关键词： Imidazoheterocycles Sulfenylation Water

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糖胶树叶挥发油化学成分研究

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化学研究 2017年第2期28卷 210-212页

作者：孔杜林林强海南医学院药学院海南海口571199 海南师范大学化学与化工学院海南海口571158

采用水蒸气蒸馏法提取糖胶树叶的挥发油.运用气质谱联用(GC-MS)技术研究海南糖胶树叶的挥发油化学成分.并采用峰面积归一化法确定各成分的相对质量分数.结果共鉴定出36种成分,占总离子流出峰面积的94.83%.糖胶树叶挥发油主要有α-蒎烯(1... 详细信息

采用水蒸气蒸馏法提取糖胶树叶的挥发油.运用气质谱联用(GC-MS)技术研究海南糖胶树叶的挥发油化学成分.并采用峰面积归一化法确定各成分的相对质量分数.结果共鉴定出36种成分,占总离子流出峰面积的94.83%.糖胶树叶挥发油主要有α-蒎烯(16.62%),2-丙烯酸丁酯(15.86%)和大根香叶烯D(13.37%).本研究可为糖胶树的进一步研究开发和利用提供基础研究数据.

关键词：糖胶树挥发油水蒸气蒸馏法 GC-MS

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科教协同在药学专业有机化学课程中的应用研究

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科技创新导报 2020年第36期17卷 231-233页

作者：陈训孔杜林海南医学院药学院海南海口571199

科教协同理念已成为当今高校打造教学研究型大学的发展目标,是教学改革发展的重要方向。而在药学专业课程中,有机化学是一门依托教学和科研相结合的基础学科。在课堂教学中引入前沿的科研成果,注重科教协同理念,不仅能够扩宽学生的知识... 详细信息

科教协同理念已成为当今高校打造教学研究型大学的发展目标,是教学改革发展的重要方向。而在药学专业课程中,有机化学是一门依托教学和科研相结合的基础学科。在课堂教学中引入前沿的科研成果,注重科教协同理念,不仅能够扩宽学生的知识面,还提高学习的积极性以及创新思维能力。本文将结合近几年在药物合成以及药物活性方面的前沿成果,介绍了如何把科研成果融入到有机化学课堂教学中的几点应用实例。

关键词：科教协同有机化学积极性创新思维能力

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钌(Ⅱ)-催化芳胺C—H键与炔丙醇的高选择性[3+2]环化反应

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有机化学 2018年第12期38卷 3242-3249页

作者：白丽丽王颖王烁今孔杜林付艳彭德乾文丽君陈训海南医学院药学院海口571199

报道了一种简便有效的Ru(Ⅱ)-催化芳胺C—H键与炔丙醇的高选择性[3+2]环化反应,能够高效构建含有羟基功能基的吲哚骨架结构,为进一步衍生更加复杂有用的药物分子提供简便的合成渠道.同时研究了该反应的动力学同位素效应,实验结果表明C—... 详细信息

报道了一种简便有效的Ru(Ⅱ)-催化芳胺C—H键与炔丙醇的高选择性[3+2]环化反应,能够高效构建含有羟基功能基的吲哚骨架结构,为进一步衍生更加复杂有用的药物分子提供简便的合成渠道.同时研究了该反应的动力学同位素效应,实验结果表明C—H键活化可能属于整个反应历程的决速步骤.

关键词：钌(Ⅱ) C-H键高选择性环化反应

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Synthesis and Characterization of α-Aminophosphonic Acids Containing Adenine

Synthesis and Characterization of α-Aminophosphonic Acids C...

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有机合成创新—产业化的新动力——中国化学会全国第三届有机合成化学与过程学术讨论会

作者： kong,dulin Wu,Luyong Wu,Mingshu~* Ma,Jingya (Key Laboratory of Tropical Medicinal Plant Chemistry of Ministry of Education,Hainan Normal University,College of Chemistry and Chemical Engineering,Hainan Normal University,Haikou 571158)

α-Aminophosphonic acids and their derivatives have drawn considerable attention in the recent years because of their unique structural features and potential biological activities,such as herbicides,insecticides, fungicides,peptidomimetics,enzyme inhibitors and antiviral agents as well as their role for antibody ***,which exists in the nucleic acid of the organism as a base,has drawn great attention of biochemists and organic synthetic chemists in recent years because of its good active biologic ***

关键词： α-aminophosphonate adenine three-component condensation reaction

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