基于问题的教学法在药物化学教学中的应用

药物化学是药学专业和制药工程专业的必修课。为提高教学质量,尝试将基于问题的教学法（PBL）应用于药物化学教学中,构建以学生为中心、发展自主学习的技能的相关教学模式,创设了适合于学生主动参与的新型教学环境,并对相应具体操作模式进行探讨。初步提出了一些评价方法,对于提高师生的教学兴趣,考察PBL教学效果具有指导意义。     

从PBL教学方法谈医学检验专业本科分析化学教学改革

作为医学检验专业分析化学教师 ,不仅要使医学检验专业的学生掌握分析化学的基本理论和应用 ,还要使学生的综合能力通过学习分析化学得到锻炼和提高 ,为分析化学和临床检验的发展培养合格人才。因此 ,深化大学阶段分析化学教学改革 ,提高分析化学教学质量刻不容缓。下面从 3个方面谈谈PBL教学方法与分析化学教学改革。1　PBL教学法及其意义　　PBL即Problem BasedLearning的缩写 ,中文译为“以问题为基础的教学法”。该方法由美国神经病学教授Barrows创立 ,与传统教学法的根本区别在于 :前者强调以学生的主动学习为主 ,在干中学 ,学生…     

PBL与LBL结合的教学模式在工科有机化学教学中的应用

分析了以问题为中心的教学模式的优缺点,提出了PBL(Problem-based Learning)教学与LBL(Lecture-based Learning)教学相结合的模式,并在制药工程专业及化学工程与工艺专业的有机化学教学中尝试开展了PBL与LBL相结合的教学模式,实践表明该教学模式有助于增强有机化学教学效果,提高教学质量。该教学模式可以在工科学生的有机化学教学中进行推广应用。     

结合PBL课例的无机化学线下对分课堂教学设计与实践*

以原电池一节教学设计为例,探索了将PBL课例融入对分课堂教学模式。教学实践表明,新教学模式激发了学生的学习兴趣,提高了学生学习的积极性和主动性,提升了课程教学效果,达到了课程教学目标。对PBL课例与对分课堂有机融合的全新课堂教学模式的建设与发展进行了展望。     

药学专业留学生分析化学实验全英文教学的体会

留学生教育已成为我国高等教育的重要组成部分,而全英文教学是无中文基础的留学生的最佳选择。分析化学实验为药学专业本科生的必修课,本文针对药学专业留学生分析化学实验课的全英文教学过程,从课程的教学安排、教材选用、教学师资、授课方式和考评方式等方面讲述了教学实践中的体会,希望为开设同类课程的全英文教学提供借鉴和参考。     

“工业分析”课程中PBL与LBL相结合的教学探讨

根据应用化学的专业特点,在"工业分析"课程中进行PBL与LBL相结合的教学探讨。通过对PBL教学模式的实施过程、应用效果、实施前提以及存在问题的论述分析,提出对综合性较强的学科采用PBL与LBL相结合教学法的必要性。特别是对学习独立性与自主性较强的高年级学生,PBL与LBL相结合的教学法在提高学生学习兴趣,增强学生分析问题的能力等方面具有一定的优势,有利于"工业分析"课堂教学质量的提高。     

基于微课的翻转课堂教学模式在分析化学实验教学中的探索

分析化学实验是大学化学实验的重要内容,是分析化学课程学习中不可缺少的组成部分。为了提高分析化学实验教学质量,提升学生动手能力、分析问题和解决问题的能力以及创新能力,解决传统教学模式存在的主要问题,对分析化学实验教学模式进行了改革探索。将以微课为基础的翻转课堂教学模式引入到分析化学实验中,激发学生的实验热情,提高学生综合实验技能,巩固基础理论知识,培养了科学研究思维,真正实现创新性人才培养目标。     

转动课堂在分析化学教学中的应用

"转动课堂"是渤海大学依据地方综合性大学的人才培养目标,借鉴国内外的课堂教学模式引申而来,将课堂精讲与师生互动紧密结合,个性化培养学生的创新能力和动手能力。本文介绍了分析化学结合学科特点及转动课堂核心理念,设计自学、精讲、互动等8个教学环节以提高课堂效率。这种课内课外协同互补的教学模式,激发了学生学习分析化学课程的热情,课堂教学质量及学生学习效果明显提高。     

以新药研发为案例的有机药物化学课程群PBL教学设计

在有机药物化学课程群中开展PBL教学改革,基于新药凯美纳的开发进行教学设计。通过凯美纳药物小分子的发现、合成设计、药学评价、新药上市等剧情把课程群间的课程内容有机地整合,从整体上加深学生对药学专业的认识,注重知识的灵活应用,达到“学有所成,学以致用”的目的;同时,PBL教学采用小组合作学习形式,培养了学生自主学习和终身学习的技能,提升了学生的团队合作意识和能力。     

国内外药学专业分析化学教材的比较

通过对近年来国内外药学专业使用的分析化学教材的比较,总结了不同教材的特点,讨论了我国药学专业使用的分析化学教材和发达国家同类教材的区别及差距,分析了今后教材的发展趋势。     

二氧化碳和丙烯直接合成甲基丙烯酸的NiPMo/TiO2催化剂的研究

用溶胶-凝胶法以磷钼酸(MPA)的镍盐溶液水解钛酸四丁酯制备了NiPMo/TiO2催化剂.使用ICP、 XRD、 TG-DTA、 IR、 TPD-MS和微反应技术研究了催化剂的化学组成、热稳定性、化学吸附性质和催化反应性能.杂多钼酸盐与TiO2通过O2-在TiO2表面发生了键合.在623 K下,杂多阴离子仍保持原有的Keggin结构.CO2在Lewis酸位Ni(Ⅱ)和Lewis碱位Ni-O-Mo的桥氧协同作用下生成CO2卧式吸附态Ni(Ⅱ)←O-(CO)←(O--Ni).丙烯有多种吸附态在催化剂上吸附.在563 K、 1 MPa和空速1500 h-1的反应条件下,丙烯的摩尔转化率为3.2%,产物MAA选择性为95%.     

Synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives

Different approaches for the synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives from simple amino acids have been investigated. A library of 33 precursors for the preparation of N-hydroxy pyrazinones was obtained in moderate to good yields.     

α-Amino acid derived enaminones and their application in the synthesis of N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates and other heterocycles

A new and simple synthesis of novel N-protected methyl 5-substituted-4-hydroxypyrrole-3-carboxylates, which exist in equilibrium with their 4-oxo tautomers, has been developed in two steps starting from N-protected α-amino acids. The key intermediates are enaminones, which can also be isolated, characterized, and used for the construction of other functionalized heterocycles, before they spontaneously decompose to pyrrole products. 4-Hydroxypyrroles are prone to partial aerial oxidation but can be efficiently alkylated or reduced to stable polysubstituted pyrrolidine derivatives.     

Specific intramolecular aromatic CH insertion of diazosulfonamides

The chemoselectivity in the intramolecular CH insertion of various diazosulfonamides has been experimentally studied. The results reveal that the aliphatic 1,4-, 1,5-, or 1,6-C(sp³)?H insertions of diazosulfonamides are not accessible, while the aromatic 1,5-C(sp²)?H insertion can be realized specifically by adjusting the diazo-adjacent group. In addition, the general chemoselectivities in the intramolecular CH insertions of diazosulfonyl compounds are summarized. Generally, diazosulfones undergo both aromatic 1,5-C(sp²)?H and aliphatic 1,5- and 1,6-C(sp³)?H insertions, while diazosulfonates undergo aliphatic 1,5- and 1,6-C(sp³)?H insertions. However, diazosulfonamides only undergo aromatic 1,5-C(sp²)?H insertion.     

A general and convenient synthesis of 4-(tosylmethyl)semicarbazones and their use in amidoalkylation of hydrogen,heteroatom, and carbon nucleophiles

A general synthesis of previously unknown semicarbazone-based α-amidoalkylating reagents, 4-(tosylmethyl)semicarbazones, has been developed. The synthesis involved three-component condensation of semicarbazones of aliphatic or aromatic aldehydes with the same or other aldehydes and p-toluenesulfinic acid. The scope and limitations of this reaction were investigated. The compounds obtained were demonstrated to be an efficient α-(4-semicarbazono)alkylating agents. They were reacted with H- (sodium borohydride), O- (sodium methylate), S- (sodium phenylthiolate), N- (pyrrolidine, sodium succinimide), P- (trialkyl phosphites), and C-nucleophiles (sodium diethyl malonate) to give the corresponding products of the tosyl group substitution, 4-substituted semicarbazones, including analogues of nitrofurazone. Among the prepared compounds tested in vitro for antibacterial and antifungal activity, three nitrofuryl-containing semicarbazones exhibited high biological activities with minimum inhibitory concentration (MIC) values of 8–32 μg/mL.     

Synthesis of novel chiral bidentate hydroxyalkyl-N-heterocyclic carbene ligands and their application in palladium-catalyzed Mizoroki–Heck couplings and asymmetric addition of diethylzinc to benzaldehyde

A small library of new chiral bidentate hydroxyalkyl-imidazolium salts 1 is conveniently synthesized on multi-gram scale from inexpensive and commercially available chiral pool amino acids. The corresponding carbenes, generated by deprotonation of imidazolium salts 1, in combination with palladium(II) chloride were tested in the Mizoroki–Heck coupling reaction. The most significant results in terms of yields and reactivities were achieved with low catalyst loading. The catalytic activities of these imidazolium salts were also investigated in the asymmetric addition of diethylzinc to benzaldehyde. The use of MgO nanoparticles as an additive in conjunction with these ligands played a crucial role in increasing the efficiency of these reactions.     

N-Heterocyclic carbene-palladacyclic complexes: synthesis,characterization and their applications in the C-N coupling and α-arylation of ketones using aryl chlorides

N-Heterocyclic carbene-palladacyclic complexes 3 were successfully achieved in a one-pot procedure under mild conditions. The structure of 3a was unambiguously confirmed by X-ray single crystal diffraction and it was an active catalyst in the Buchwald-Hartwig amination and α-arylation of ketones even at very low catalyst loadings (0.01?mol%).     

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated as by-products of some experiments.     

Iodine-mediated oxidative Pictet-Spengler reaction using terminal alkyne as the 2-oxoaldehyde surrogate for the synthesis of 1-aroyl-β-carbolines and fused-nitrogen heterocycles

An efficient iodine-mediated oxidative Pictet-Spengler reaction in dimethyl sulphoxide (DMSO) using terminal alkynes as the 2-oxoaldehyde surrogate for the synthesis of aryl (9H-pyrido[3,4-b]indol-1-yl)methanones is described. The scope of the protocol includes the total synthesis of Fascaplysin, Eudistomins Y₁ and Y₂. The methodology is extended for preparing pyrrolo[1,2-a]-quinoxaline and indolo[1,5-a]quinoxaline derivatives. The utility of 1-aroyl-β-carbolines was demonstrated by performing palladium-catalyzed β-carboline directed ortho-C(sp2)-H functionalization of the phenyl ring with thiomethyl (SMe) group using DMSO as source and for accessing 4-aryl-canthin-6-ones.     

Facile synthesis of bicyclic 1-arylpyrazol-5-ones

In this Letter, we described a facile method for constructing fused bicyclic 1-arylpyrazol-5-one ring system. We employed various methylene-containing carboxylic acids as the substrates and proved that the pyrazolone ring closure requires activated methylene group in intermediate II. Accordingly, a series of structurally diversified, fused bicyclic 1-arylpyrazol-5-ones was prepared in moderate to high yields using the requisite substrates.