Facile Synthesis of 2H-Pyrroles: Combination of Gold Catalysis and Lewis Acid Catalysis

报道了利用金催化与铜催化相结合合成5-氨基-2H-吡咯的方法.首先通过均相金催化异恶唑与炔酰胺反应生成α-亚胺金卡宾中间体,再经[3+2]环加成反应合成并分离出5-氨基-3H-吡咯,然后通过铜催化的去酰基化和基团迁移反应来实现3H-吡咯向2H-吡咯的转化.该方法不但操作简单、反应条件温和、官能团兼容性良好,而且还能进行克量级放大.这项研究为合成具有重要生物活性的5-氨基-2H-吡咯化合物提供了广谱实用的合成方法.A two-step synthesis of 5-amino 2H-pyrroles using gold and copper catalysis was presented. Firstly, 5-amino 3H-pyrroles were synthesized by gold-catalyzed formal [3+2] cycloaddition between ynamides and isoxazoles via α-imino gold carbene intermediate. The following Lewis acid-triggered decarbonylation and group migration results in the formation of 5-amino 2H-pyrroles. Other notable features of this method include the simple procedure, the mild reaction conditions and compatibility with a broad range of functional groups. Thus, this protocol provides a practical and general solution for the synthesis of 5-amino 2H-pyrroles. Accordingly, isoxazole 2(2.0 equiv., 0.6 mmol) and Ph3 PAu NTf2(5 mol%) were added to a suspension of the ynamide 1(1.0 equiv., 0.3 mmol) in DCM(3.0 m L) at room temperature. The reaction mixture was then stirred at r.t. and the progress of the reaction was monitored by TLC. The reaction typically took 2 h. Upon completion, the mixture was quenched with pyridine, concentrated and purified by chromatography on silica gel, using an eluent of petroleum ether/ethyl acetate(5/1, V/V), to afford 3H-pyrrole 3. Then, 3H-pyrrole 3 and Cu(OTf)2(10 mol%) were dissolved in DCM(3 m L) and stirred at room temperature for 6 h. The residue was purified by column chromatography on silica gel, using an eluent of petroleum ether/ethyl acetate(3/1, V/V), to afford the desired 2H-pyrrole 4. Under this condition, a variety of differently substituted ynamides 1 and isoxazoles 2 work well to provide the corresponding 2H-pyrroles 4a~4l in moderate to good overall yields. But N-(4-methoxybenzyl)-N-(phenylethynyl)methanesulfonamide 1a reacts with 4-(3-bromophenyl)-3,5-dimethylisoxazole 2d poorly under this condition, affording product 4h in only 33% yield. These results indicate that this method has certain universality, but the reaction is influenced by the substituents to some extent. Notably, the scalability and preparative utility of the developed methodology was exemplified by the fact that the desired product 4a was obtained without a significant loss in yield when the reaction was scaled up to 5 mmol. Also a plausible mechanism is proposed and we tend to believe that the reaction is featured by an α-imino gold carbene intermediate.国家自然科学基金(No.21272191);; 福建省杰出青年科学基金(No.2015J06003);; 国家基础科学人才培养基金(No.J1310024)资助~

空间特征关联性研究——以厦门鼓浪屿龙头路为例

本文基于整体空间和局部空间的调研,以鼓浪屿龙头路为案例进行空间特征的量化分析。研究首先对现有建筑空间和道路布局进行描述,通过空间句法分析现有街道空间、视线的活跃程度。同时,通过聚类分析分类区域内单体建筑空间要素,探究建筑单体对现有空间活力产生的影响,揭示局部空间特征与整体空间特征的关联性。研究有助于加强空间量化分析对现有空间活化的利用。福建省科技计划项目“厦、金八·二三炮战遗址整体性保护研究”(编号:2018R0091

On the Public Interests of Society in International Investment Law

在传统国际投资条约与国际投资争端实践中，关于社会公共利益的内容主要是针对资本输入国征收外国私人投资者财产的情形。但是随着国际投资条约与国际投资争端实践的发展，对于社会公共利益的保护逐渐突破征收条款的禁锢，并且对国际投资法律体系有着深远的影响。本文之研究以国际投资条约的社会价值追求为主线，主要从两个方面对社会公共利益进行探讨：一方面从国际投资条约的角度，另一方面从国际投资争端实践的角度，以便较为全面地对国际投资法中涉及的社会公共利益问题进行研究。传统的国际投资条约或者处理国际投资争端的模式已经不适应现代国际投资的发展与演化。所以，无论是国际投资条约还是国际投资争端解决程序都需要完善。 传统的国...The content regarding the public interests of society mainly reflected in the expropriation of foreign investors’ property of capital importing countries in the traditional practices of international investment treaties and international investment disputes. However, with the development of practices in international investment treaties and international investment disputes, the public interests o...学位：法学博士院系专业：法学院法律系_国际法学(含国际公法、国际私法、国际经济法)学号：1362008015004

Research on the Clinical Pathway PDCA Continuous Improvement System Based on the Theory of Feedback Closed-loop Control System

运用控制论方法，将控制理论领域反馈的闭环控制法、管理学的PDCA循环等方法运用于信息系统的整合建设，建立电子病历一电子医嘱一临床路径一医院管理信息系统的“全闭环”临床路径执行和反馈体系，建立了疾病诊疗规范制定、临床操作服务、过程质量监管三位一体的医疗服务安全质量监测与持续改进闭环体系，临床路径信息管理平台对加强医疗服务安全动态监管，促进科学化、精细化、专业化管理，改善服务水平，提高效率具有不可或缺的重要作用。With the method of control theory, the feedback closed loop control method in the field of control theory, PDCA circulation of management and other methods are applied to the integrative construction of information system. The ＂closed loop＂ clinical pathway implementation and feedback system of electronic medical records-electronic medical advice-clinical pathway- hospital management information system is established. The medical service safety quality monitoring and continuous improvement closed-loop system integrating disease diagnosis and treatment specification formulation, clinical operation service and process quality supervision is set up. The clinical path information management platform has an indispensable important role on strengthening the dynamic supervision of medical service security, promoting scientific, refined and professional management, and improving the service level and eficiency.国家自然科学基金面上项目一大数据驱动的抗菌药物使用与管理决策优化研究（编号：71672160

[[alternative]]Development of Instructional Material (III)

計畫編號：NSC91-2520-S032-003研究期間：200208~200307研究經費：507,000[[sponsorship]]行政院國家科學委員

不同季节垃圾填埋场周围重金属污染特征及评价

采集漳州市某生活垃圾填埋场周围冬夏两季的地表水(包括渗滤液)、土壤以及植物样品,分析9种重金属总量的季节性变化.结果表明,冬季地表水中Zn和As,土壤和植物中的Cd和As的含量均大于夏季,而夏季波动性强于冬季;夏季渗滤液中总Hg的含量明显高于冬季,其余变化不明显.地表水重金属含量均低于地表水环境质量Ⅴ类标准限值,渗滤液中所有重金属含量均低于污水排放二级标准限值.土壤中重金属Cd、As和Pb的污染最重,已达到重度污染,冬季的污染明显高于夏季.冬季植物富集能力强于夏季,细叶芒对Cd的富集能力较强,可作为重金属污染修复的先锋植物.环保公益性行业科研专项(201509054)资助~

Research on International Competitiveness of Chinese Manufacturing Using the Method of Unit Labor Cost

计算、比较中国与主要出口竞争国的单位劳动力成本(ulC),发现中国制造业仍然具有较大的国际竞争优势,原因是多年来制造业劳动生产率增速明显快于工资增速,使单位劳动成本保持下降趋势。相对单位劳动力成本(rulC)的比较结果显示,即使不考虑提高工资将促使劳动生产率进一步提升以及基础设施、国内市场、政治环境等方面的优势,在现有劳动生产率水平上,中国制造业仍能够承受约50%的劳动报酬上升。用购买力平价调整后的ulC数据说明,尽管汇率低估在一定程度上强化了中国制造业国际竞争优势,但2005年汇率改革以来,这种附加优势已基本消失。Through calculating and comparing the Unit Labor Cost(ULC) and Relative Unit Labor Cost(RULC) between China and major export competition countries,this article found that Chinese manufacturing still had a large international competitive advantage,and the reason lied in that the growth rate of labor productivity of manufacturing workers was significantly faster than wage growth,which made the downward trend in unit labor cost.Furthermore,the comparison of RULC shows that even without considering that the higher wages will lead further improvement of labor productivity and the advantages in infrastructure,domestic market,and political environment,China is still able to withstand about 50% of the rise in labor compensation under the existing level of labor productivity.In addition,by calculating the adjusted ULC data with purchasing power parity,this paper revealed that although the exchange rate which had been undervalued strengthened the international competition advantage of Chinese manufacturing to some extent,this additional advantage has disappeared since the reform of the RMB exchange in 2005

应对中美贸易战升级应加快经济增长动能转换

与中美贸易争端相比,国内经济增长动能转换对于保持中国经济的持续稳定增长,更为重要。经济增长动能转换,以坚持市场取向的全面深化改革为前提。目前经济增长新动能没有形成,集中体现在2016年民营投资出现断崖式下滑之后,至今仍未恢复此前的增长态势。国家社会科学基金重大项目《需求结构转换背景下提高消费对经济增长贡献研究》(15ZDC011);;教育部专项课题《我国经济发展动力变革问题研究》(18JF097