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t-BuOLi Catalyzed Esterification of N-Benzyl-N-Boc-amides with Carbohydrates
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作者 Ye Danfeng Xu Bing Wan Yunhui 《有机化学》 SCIE CAS CSCD 北大核心 2024年第9期2924-2932,共9页
Based on a strategy of ground-state destabilisation of the N—C bond,a general protocol for the esterification of amides with carbohydrates was reported.This protocol offers mild reaction conditions,excellent yields,a... Based on a strategy of ground-state destabilisation of the N—C bond,a general protocol for the esterification of amides with carbohydrates was reported.This protocol offers mild reaction conditions,excellent yields,and broad substrate compatibility,thereby demonstrating great potential for the synthesis of glycoconjugates.Additionally,this method provides an alternative approach for addressing the challenging task of esterifying sterically hindered secondary hydroxyl group of carbohydrates and paving the way for advancements in carbohydrate-based pharmaceuticals. 展开更多
关键词 t-BuOLi N-benzyl-N-Boc-amides ESTERIFICATION glycoconjugates
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基于制剂原料物理特性的止颤颗粒干法制粒处方与工艺优选 被引量:20
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作者 杨秀娟 洪燕龙 +4 位作者 阮克锋 冯怡 杜若飞 曹韩韩 张雪 《中国实验方剂学杂志》 CAS 北大核心 2013年第4期27-30,共4页
目的:考察止颤颗粒制剂原料的物理特性,优选止颤颗粒的处方及成型工艺。方法:用粉体综合测试仪、激光粒度分布仪等测定止颤颗粒制剂原料的休止角、压缩度、含水量及黏聚力等;以颗粒成型率、脆碎度和外观评分为指标,采用单因素与正交试... 目的:考察止颤颗粒制剂原料的物理特性,优选止颤颗粒的处方及成型工艺。方法:用粉体综合测试仪、激光粒度分布仪等测定止颤颗粒制剂原料的休止角、压缩度、含水量及黏聚力等;以颗粒成型率、脆碎度和外观评分为指标,采用单因素与正交试验筛选止颤颗粒最佳辅料与最佳制粒工艺参数。结果:制剂原料的休止角31°,黏聚力1.36 kpa,压缩度33.96%,含水量4.84%,粒径分布37.96μm;最佳处方组成为84.0%浸膏粉,1.0%硬脂酸镁,0.7%三氯蔗糖,0.5%红茶香精,13.8%糊精;干法制粒最优工艺参数为水平转速30 r.min-1,辊轮转速5 r.min-1,辊轮压力5 MPa。结论:制剂原料的物理特性研究可指导干法制粒制剂处方的筛选;所制得的颗粒载药量高、成型率较高、外观好、口感好,优选的干法制粒工艺稳定可行。 展开更多
关键词 止颤颗粒 物理特性 辅料筛选 干法制粒
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Phytochemistry,biological properties and quality control of Chuanxiong Rhizoma:a review 被引量:4
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作者 Jinhui Shi Ruiyue Li +1 位作者 Siyu Yang Hongmei Zhang 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2020年第11期753-779,共27页
Chuanxiong Rhizoma is a widely used Chinese herbal medicine in the past 2000 years.Chuanxiong Rhizoma is composed of volatile oils,phthalide lactones,phenolic acids,polysaccharides and other compounds.To date,more tha... Chuanxiong Rhizoma is a widely used Chinese herbal medicine in the past 2000 years.Chuanxiong Rhizoma is composed of volatile oils,phthalide lactones,phenolic acids,polysaccharides and other compounds.To date,more than 149 compounds in Chuanxiong Rhizoma have been isolated and identified,and some of them have been reported to possess promising biological properties on cardiovascular and central nervous system disorders besides their anti-cancer and antioxidant effects.Modulation of inflammatory mediators and apoptotic factors are believed to contribute to its bioactivities.Analytical methods,such as HPLC,GC and UPLC,are employed for qualitative evaluation of Chuanxiong Rhizoma.In this work,harvest period,growing habitat,processing method and storage,which can affect the quality of Chuanxiong Rhizoma,were also discussed.Comprehensive quality control methods should be developed to ensure the safety,quality and efficacy use of Chuanxiong Rhizoma.Herein,we collected and analyzed the literature of Chuanxiong Rhizoma published on CNKI,ScienceDirect,Springer link,Wiley and PubMed in past two decades,and up-to-date information of Chuanxiong Rhizoma was provided in this paper.We suggested ligustilide,butylidenephthalide and total senkyunolides as the chemical markers to evaluate the quality of Chuanxiong Rhizoma.Additionally,the influences of soil conditions and processing methods on Chuanxiong Rhizoma as future research perspectives should also be further assessed. 展开更多
关键词 Chuanxiong Rhizoma(CXR) PHYTOCHEMISTRY Biological property Quality control
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Determination of free fatty acids in rabbit plasma by GC-MS after trimethylsilylation derivatization 被引量:2
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作者 Jialin Du Liangjiu Yang +3 位作者 Kezhao Wei Can Gong Jianping Gao Xu Xu 《Journal of Chinese Pharmaceutical Sciences》 CAS CSCD 2020年第6期411-421,共11页
In the present study, free fatty acids(FFAs, including palmitic acid, stearic acid, oleic acid, linoleic acid and arachidonic acid) in rabbit plasma were determined by gas chromatography-mass spectrometry(GC-MS) after... In the present study, free fatty acids(FFAs, including palmitic acid, stearic acid, oleic acid, linoleic acid and arachidonic acid) in rabbit plasma were determined by gas chromatography-mass spectrometry(GC-MS) after trimethylsilylation derivatization using N,O-bis(trimethylsilyl)trifluoroacetamide(BSTFA) – trimethylchlorosilane(TMCS) as derivatization reagent. The experimental conditions, including extraction and silylation reaction, were investigated. The method was experimentally validated. The linearity between fatty acids’ peak areas and their concentrations was obtained with the corelative coefficient(r2) all more than 0.999, and the recoveries were between 82% and 111%. The intra-day variations of FFAs’ in plasma samples at different concentrations were all less than 6%. FFA analysis results of 16 rabbit plasma samples showed that the method could be well applied in the determination of plasma samples in vivo. In contrast to the traditional method of FFA derivatization, the established trimethylsilylation method presented simplicity, high specificity, and completely free from the interference of the esterified fatty acid, such as triacylglyceride. The method could be applied for analyzing FFA profiles in the clinical laboratory or pharmacological research. 展开更多
关键词 Free fatty acid TRIMETHYLSILYLATION DERIVATIZATION Gas chromatography-mass spectrometry Rabbit plasma
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