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Microwave-activated Synthetic Route to Various Biologically Important Heterocycles Involving Transition Metal Catalysts 涉及过渡金属催化剂的微波激活合成各种重要生物杂环的途径
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-12-08 DOI: 10.2174/0122133356267427231120062925
Soumyadip Basu, C. Mukhopadhyay
This study incorporates the assembly of development methodologies of microwave-acti-vated protocol involving transition metal catalysts for the synthesis of numerous biologically im-portant heterocycles during the past few years. Herein, it highlights the potential of transition metal salts as catalysts in multicomponent reactions performed under microwave conditions for the for-mation of oxygen, nitrogen, and sulphur-containing bioactive heterocycle moieties. Microwave-activated organic synthesis has been well-utilized as an alternative to conventional methodology in pharmaceutical companies due to its potential to significantly improve the rate and consequently diminish the time span of the synthetic process. The traditional methods involving transition metal catalysts for synthesizing bioactive heterocyclic molecules are prolonged and, thus, difficult to meet the requirements for the timely supply of these important compounds. In our review, our main focus is on integrating such synthetic strategies involving transition metal catalysis with a microwave-activated multicomponent approach for developing bioactive heterocycles.
本研究汇总了过去几年中涉及过渡金属催化剂的微波作用程序的开发方法,用于合成多种具有重要生物学意义的杂环。在这里,它强调了过渡金属盐作为催化剂在微波条件下进行的多组分反应中用于合成含氧、氮和硫的生物活性杂环分子的潜力。微波活化有机合成法可显著提高合成速率,从而缩短合成过程的时间跨度,因此已被制药公司广泛用作传统方法的替代方法。使用过渡金属催化剂合成生物活性杂环分子的传统方法耗时较长,因此难以满足及时供应这些重要化合物的要求。在我们的综述中,我们主要关注的是将这种涉及过渡金属催化的合成策略与微波活化多组分方法相结合,以开发具有生物活性的杂环化合物。
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引用次数: 0
One-step Synthesis of Deep Eutectic Solvents and dissolution of their Kraft Lignin 一步合成深共晶溶剂并溶解其牛皮纸木质素
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-12-08 DOI: 10.2174/0122133356264245231120053530
Omar Merino Pérez, Ricardo Cerón-Camacho, Rafael Martinez Palou
Lignin is a very abundant biopolymer with great potential to produce other high-value polymers with aromatic groups. Its valorization has been limited principally by its poor solubility in conventional organic solvents, which makes it difficult to deconstruct or transform it into other products with higher added value. In this work, we describe a one-pot procedure to prepare vari-ous Deep Eutectic Solvents and study their ability to dissolve Kraft lignin with the aid of micro-wave dielectric heating efficiently.Lignin is a widely available aromatic biopolymer that is largely discarded or used as a low-value fuel when separated in paper production processes, so researchers are engaged in the development of lignin dissolution processes that allow its easy deconstruction and transfor-mation into other products with higher added value.The main objective of this work is to find deep eutectic solvents capable of dissolving significant quantities of lignin with the aid of microwaves as a heating source.The present work developed a simple, fast, and efficient method to dissolve lignin using Deep Eutectic Solvent/acetonitrile as solvents and irradiation by dielectric microwave heating.Most of the DESs studied achieved significant dissolution of purchased lignin with com-mon organic solvents by employing microwave irradiation as the heating method.Some DESs studied in this work are good alternatives as solvents for lignin due to the solvent option of simple preparation from renewable precursors from biomass, such as glyc-erol, choline chloride, and urea, of low toxicity and cost for this application. The effectiveness of these systems appears to be based on molecular recognition by hydrogen bonding interactions involving the three species that make up the eutectic and the hydroxyl groups of the lignin. These solvents can be recovered and recycled.
木质素是一种非常丰富的生物聚合物,具有生产其他带有芳香基团的高价值聚合物的巨大潜力。木质素在传统有机溶剂中的溶解度较低,使其难以解构或转化为其他具有更高附加值的产品,从而限制了其价值的提升。在这项工作中,我们介绍了制备各种深共晶溶剂的一锅程序,并研究了它们在微波介电加热的帮助下高效溶解牛皮纸木质素的能力。木质素是一种广泛存在的芳香族生物聚合物,在造纸过程中分离出来后大多被丢弃或用作低价值燃料,因此研究人员致力于开发木质素溶解工艺,使其易于解构并转化为其他具有更高附加值的产品。本研究开发了一种简单、快速、高效的溶解木质素的方法,使用深共晶溶剂/乙腈作为溶剂,并通过介质微波加热进行辐照。所研究的大多数 DES 通过使用微波辐照作为加热方法,实现了用普通有机溶剂大量溶解所购买的木质素。这项工作中研究的一些 DESs 是木质素溶剂的良好替代品,因为这些溶剂可从生物质中的可再生前体(如甘油醇、氯化胆碱和尿素)中简单制备,毒性低且成本低。这些系统的有效性似乎是基于组成共晶的三种物质与木质素羟基之间的氢键相互作用所产生的分子识别。这些溶剂可以回收和循环使用。
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引用次数: 0
Infusion of Magnetic Nanocatalyst to Microwave Propped Synthesis ofBioactive Azaheterocycles 将磁性纳米催化剂注入微波支撑的生物活性氮杂环合成中
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-12-04 DOI: 10.2174/0122133356269940231116134734
Pranali Hadole, Sampat R. Shingda, Aniruddha Mondal, Kundan Lal, R. Chaudhary, Sudip Mondal
Microwave-assisted synthesis is a powerful tool in organic chemistry, providing arapid and efficient method for the synthesis of bioactive heterocycles. The application of microwaves significantly reduces reaction times and increases percentage yields with high purity of thefinal product. To make the synthetic protocol greener, the application of the magnetic nanocatalyst is a rapidly growing area of interest nowadays. Magnetic nanocatalyst, with its unique features like magnetic separable facile recovery from the reaction media heterogeneously, makes theoverall synthetic strategy cleaner, faster, and cost-effective. Aiming this, in the present review,we will focus on the infusion of Magnetic nanocatalyst to microwave-assisted synthesis of various classes of azaheterocyclic compounds, including pyridines, pyrimidines, quinolines, and benzimidazoles. The synthetic methodologies involved in the preparation of these heterocycles arehighlighted, along with their biological activities. Furthermore, in this review, the most recentand advanced strategies to incorporate nanocatalysts in the microwave-assisted synthesis of natural products containing azaheterocyclic moieties in drug discovery programs are elucidated indetail, along with the incoming future scope and challenges
微波辅助合成是有机化学中一种强有力的工具,为合成具有生物活性的杂环化合物提供了一种快速、高效的方法。微波的应用大大减少了反应时间,提高了最终产品的纯度。为了使合成方案更加环保,磁性纳米催化剂的应用是当今人们感兴趣的一个快速增长的领域。磁性纳米催化剂以其独特的特点,如磁性可分离易于从反应介质中非均质回收,使整体合成策略更清洁,更快速,更具成本效益。为此,本文将重点介绍磁性纳米催化剂在微波辅助下合成各种杂环化合物的研究进展,包括吡啶类、嘧啶类、喹啉类和苯并咪唑类。重点介绍了这些杂环化合物的合成方法及其生物活性。此外,本文还详细阐述了在药物发现计划中,将纳米催化剂纳入微波辅助合成含氮杂环的天然产物的最新和先进策略,以及未来的范围和挑战
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引用次数: 0
Microwave-assisted Synthesis of Bioactive Six-membered O-heterocycles 微波辅助合成具有生物活性的六元 O 型杂环
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-12-01 DOI: 10.2174/0122133356269695231120095457
Aramita De, Subhankar Sarkar, A. Majee
Microwave radiation has been utilised since the late 1970s as an alternativethermal energy source for chemical reactions. Initially used in inorganic chemistry, itspotential for organic chemistry was revealed in 1986. Convertion of electromagneticenergy into heat, with frequencies ranging from 0.3-300 GHz using microwave irradiation, is an efficient heating method. The microwave heating method has significantpotential for industrial processes, reducing reaction times and enhancing yields and selectivity. It finds applications in peptide and organic synthesis, materials science, polymer chemistry, biochemical processes, and nanotechnology. Microwave-assisted organic synthesis is environmentally friendly and beneficial for producing bioactive heterocyclic compounds. Oxygen-containing heterocycles are abundant and possess various biological functions, making them essential for developing new drugs. Microwavetechnology facilitates the synthesis of these compounds, including bioactive six-membered o-heterocycles such as pyrones, oxazolones, furanones, oxetanes, oxazolidinones, and dioxetanes. By utilizing modern organic transformations, microwave-assisted chemistry enhancesthe efficiency of synthetic processes, leading to the discoveryof more beneficial molecules. The review provides an up-to-date analysis of the synthesis and medicinal properties of O-heterocycles, emphasizing the strengths and needsof this field. It guides researchers, facilitating microwave-assisted green synthesis reactions and offering a flexible platform for forming bioactive heterocyclic rings.
自20世纪70年代末以来,微波辐射已被用作化学反应的替代热能来源。最初用于无机化学,1986年发现了它在有机化学中的潜力。利用微波辐射将电磁能转化为热能,频率在0.3-300 GHz之间,是一种有效的加热方法。微波加热方法在工业过程中具有显著的潜力,可以缩短反应时间,提高收率和选择性。它在多肽和有机合成、材料科学、聚合物化学、生化过程和纳米技术等领域都有应用。微波辅助有机合成是一种环境友好、有利于生产具有生物活性的杂环化合物的方法。含氧杂环化合物种类丰富,具有多种生物功能,是开发新药必不可少的物质。微波技术促进了这些化合物的合成,包括具有生物活性的六元o杂环化合物,如吡咯酮、恶唑酮、呋喃酮、氧烷、恶唑烷和二氧烷。通过利用现代有机转化,微波辅助化学提高了合成过程的效率,导致发现更多有益的分子。本文综述了o-杂环化合物的合成和药用性能的最新研究进展,强调了该领域的优势和需求。它指导研究人员,促进微波辅助绿色合成反应,并为形成生物活性杂环提供灵活的平台。
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引用次数: 0
Microwave-Assisted Solid Phase Synthesis of Different Peptide Bonds: Recent Advancements 微波辅助固相合成不同肽键的研究进展
Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-10-31 DOI: 10.2174/0122133356271504231020050826
Munna Mukhia, Kiran Pradhan, Kinkar Biswas
Abstract: Peptides are important as drugs and biologically active molecules. The synthesis of pep-tides has gathered considerable attention in recent years due to their various attractive properties. Conventional peptide synthesis is tedious and requires hazardous reagents and solvents. Micro-wave-assisted solid-phase peptide synthesis has several advantages compared with conventional batch synthesis. Herein, we have discussed various microwave-assisted solid-phase peptide bond synthesis methods developed over the last five years. Peptides are categorized into four groups - small, medium, large, and cyclic based on their length and structural characteristics to make it easier to understand. This review article also discusses the scope and limitations of microwave-assisted solid-phase peptide synthesis.
摘要:肽是重要的药物和生物活性分子。肽的合成由于其各种吸引人的性质,近年来引起了人们的广泛关注。传统的肽合成是繁琐的,需要危险的试剂和溶剂。微波辅助固相肽合成与传统的间歇合成相比具有许多优点。在这里,我们讨论了各种微波辅助固相肽键合成方法在过去的五年发展。为了便于理解,根据肽的长度和结构特征,将其分为小、中、大、环状四类。综述了微波辅助固相肽合成的范围和局限性。
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引用次数: 0
Microwave-assisted Synthesis of Heterocycles and their Anti-cancer Activities 微波辅助合成杂环化合物及其抗癌活性
Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-10-12 DOI: 10.2174/0122133356264446230925173123
Sasadhar Majhi, Pankaj Kumar Mondal
Abstract: One of the most efficient non-conventional heating methods is microwave irradiation. In organic synthesis, microwave irradiation has become a popular heating technique as it enhances product yields and purities, reduces reaction time from hours to minutes, and decreases unwanted side reactions. Microwave-assisted organic synthesis utilizes dielectric volumetric heating as an alternative activation method, which results in rapid and more selective transformations because of the uniform heat distribution. Heterocyclic compounds have a profound role in the drug discovery and development process along with their applications as agrochemicals, fungicides, herbicides, etc., making them the most prevalent form of biologically relevant molecules. Hence, enormous efforts have been made to flourish green routes for their high-yielding synthesis under microwave irradiation as a sustainable tool. Among the different clinical applications, heterocyclic compounds have received considerable attention as anti-cancer agents. Heterocyclic moieties have always been core parts of the development of anti-cancer drugs, including market-selling drugs, i.e., 5-fluorouracil, doxorubicin, methotrexate, daunorubicin, etc., and natural alkaloids, such as vinblastine and vincristine. In this review, we focus on the developments in the microwave-assisted synthesis of heterocycles and the anti-cancer activities of particular heterocycles.
摘要:微波辐射是一种最有效的非常规加热方法。在有机合成中,微波辐射已成为一种流行的加热技术,因为它可以提高产品的产量和纯度,将反应时间从几小时缩短到几分钟,并减少不必要的副反应。微波辅助有机合成利用介质体积加热作为一种替代的活化方法,由于热分布均匀,导致快速和更具选择性的转化。杂环化合物在农药、杀菌剂、除草剂等方面的应用在药物的发现和开发过程中具有深远的作用,使其成为最普遍的生物相关分子形式。因此,人们已经做出了巨大的努力,以繁荣绿色路线,在微波辐射下高产合成它们作为一种可持续的工具。在不同的临床应用中,杂环类化合物作为抗癌药物受到了广泛的关注。杂环基团一直是抗癌药物开发的核心部分,包括市场销售的药物,如5-氟尿嘧啶、阿霉素、甲氨蝶呤、柔红霉素等,以及天然生物碱,如长春花碱、长春新碱。本文主要综述了微波辅助合成杂环化合物的研究进展及特定杂环化合物的抗癌活性。
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引用次数: 0
Microwave Facilitated Discovery of Substituted 1,2,4-triazaspiro[4.5]dec-2-en-3-amines: Biological and Computational Investigations 微波促进取代1,2,4-三氮杂螺[4.5]癸-2-烯-3-胺的发现:生物学和计算研究
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-08-18 DOI: 10.2174/2213335610666230818092826
Parth P. Patel, N. Patel, M. S. Tople, V. M. Patel, Mitesh B. Solanki
Tuberculosis is an effectual infectious disease caused by the spread of tubercular bacteria within the lungs via droplets of coughs and sneezes. In 2021, 1.6 million people died due totuberculosis, which is the 13th leading killer disease and 2nd leading after COVID-19 infectious disease.Many drugs are available as antitubercular drug, but still, requires more efficacious drug molecules with lower toxicity, side effects and small-sized molecules. To fulfill said prospective, computational study such as molecular docking and ADMET studies guides towards an ideal drug molecule with small -sized, unique spiro structures.Conventional and microwave-initiated Reaction of cyclohexanone, hydrazine carbothioamide, and 2-amino-4-methoxy-6-methyl-1,3,5-triazine affords compound 1, which is subjected to the Schiff base reaction with diverse aldehydes. All structures are defined using IR, 1H NMR, 13C NMR, and mass spectroscopy. The entire series is exposed to in vitro antibacterial and antitubercular and in silico molecular docking and ADMET studies.Compounds 2c and 2b have been established to be potential antibacterial agents, whereas compounds 2d, 2e, 2j, 2k and 2l are extremely effective against tubercular strains. Furthermore, molecular docking of related molecules is performed, and compounds 2d, 2e, 2j, 2k, and 2l have higher affinities toward antitubercular proteins. ADMET parameters such as water solubility, SA score, PCaco2 value, and TPSA values are satisfactory.The microwave method has been proven to be a greener method as compared to the conventional heating method. Comparative results of in vitro analysis are obtained with referenced antibacterial drugs and antitubercular drugs. In silico observations supports their in vitro assessments. Appraisal obtained from the ADMET study leads to the formation of ideal drug molecules.
结核病是一种有效的传染病,由结核细菌通过咳嗽和打喷嚏的飞沫在肺部传播引起。2021年,有160万人死于结核病,结核病是第13大致命疾病,仅次于COVID-19传染病。抗结核药物有很多,但仍需要更有效、毒性、副作用更小、分子更小的药物分子。为了实现上述预期,分子对接和ADMET研究等计算研究指导了具有小尺寸,独特螺旋结构的理想药物分子。环己酮、肼碳硫酰胺和2-氨基-4-甲氧基-6-甲基-1,3,5-三嗪的常规反应和微波引发反应得到化合物1,该化合物1与多种醛发生席夫碱反应。所有的结构都是用IR, 1H NMR, 13C NMR和质谱来定义的。整个系列都暴露在体外抗菌和抗结核以及硅分子对接和ADMET研究中。化合物2c和2b已被确定为潜在的抗菌药物,而化合物2d、2e、2j、2k和2l对结核菌株非常有效。进一步对相关分子进行分子对接,发现化合物2d、2e、2j、2k和2l对抗结核蛋白具有较高的亲和力。ADMET参数如水溶性、SA评分、pacoo2值、TPSA值均令人满意。与传统的加热方法相比,微波方法已被证明是一种更环保的方法。体外分析结果与参考抗菌药物和抗结核药物比较。计算机观察支持他们的体外评估。从ADMET研究中获得的评价导致了理想药物分子的形成。
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引用次数: 0
Ultrasonic study of novel polymer dextran in aqueous media at 12 MHz 新型高分子右旋糖酐在12MHz水介质中的超声研究
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-08-10 DOI: 10.2174/2213335610666230810094605
Subhraraj Panda
The characteristics of matter and the dynamics of molecular processes are examined by acoustic approaches. The primary techniques in molecular acoustics are the measurement of sound speed and sound absorption, as well as the relationship between these quantities and different physical variables including pressure, temperature, and wave frequency. Molecular acoustics emerged as a separate field in the 1930s. When it was discovered that many substances disperse the speed of sound during the transmission of sound waves through them and that the classical law, which states that the coefficient of absorption is proportional to the square of the frequency, however, it does not adequately describe how sound is absorbed.The ultrasonic technique is employed because it is one of the most popular techniques, which is very easy to use, and provides precise velocity results. With careful analysis of the results, the correlation between solute and solvent was discovered. In the pharmaceutical, agricultural, and cosmetics industries, dextran and its derivatives from a few select strains have found a wide range of uses. This is why we have chosen it for our study. For assessing the impact of temperature and concentration on the aqueous medium containing the polymer dextran, ultrasonic properties are crucial. Pycnometer, Ostwald viscometer, and ultrasonic interferometer were used respectively to measure density (ρ), viscosity (η), and ultrasonic speed (u) at "303 K, 308 K, 313 K, 318 K, and 323 K." The experimental parameters are used to determine the acoustic parameters "adiabatic compressibility, Intermolecular free length, relaxation time, acoustic impedance, and Gibb's free energy".To measure the density, viscosity, and ultrasonic velocity of the solution using a pycnometer, an Ostwald's viscometer, and an ultrasonic interferometer, and to calculate the thermo acoustical parameters based on the measured parameters.Applications for examining the physico-chemical behaviour of aqueous dextran using ultrasound include understanding the nature of molecular interactions.It was investigated how concentration and temperature affected the thermoacoustic characteristics of aqueous dextran. Hydrogen bonds, charge transfer complexes, and the dissolution of hydrogen bonds and complexes are only a few examples of the forces that exist between molecules and how the analysis has interpreted their nature. Weak intermolecular forces exist.Recent developments in ultrasonic techniques have made them an effective tool for evaluating information regarding the physical and chemical behaviour of liquid molecules.
物质的特性和分子过程的动力学通过声学方法进行了研究。分子声学的主要技术是测量声速和吸声,以及这些量与不同物理变量(包括压力、温度和波频率)之间的关系。分子声学在20世纪30年代作为一个独立的领域出现。然而,当人们发现许多物质在声波传播过程中会分散声速,而经典定律规定吸收系数与频率的平方成正比时,它并不能充分描述声音是如何被吸收的。之所以采用超声波技术,是因为它是最流行的技术之一,使用起来非常容易,并且可以提供精确的速度结果。通过对结果的仔细分析,发现了溶质和溶剂之间的相关性。在制药、农业和化妆品行业,葡聚糖及其从一些精选菌株中提取的衍生物有着广泛的用途。这就是为什么我们选择它进行研究。为了评估温度和浓度对含有聚合物右旋糖酐的水性介质的影响,超声性质是至关重要的。分别使用比重瓶、奥斯特瓦尔德粘度计和超声波干涉仪测量密度(ρ)、粘度(η)、,以及在“303 K、308 K、313 K、318 K和323 K”下的超声速度(u)。实验参数用于确定声学参数“绝热压缩性、分子间自由长度、弛豫时间、声阻抗和吉布自由能”。使用比重瓶、奥斯特瓦尔德粘度计测量溶液的密度、粘度和超声速度,以及超声波干涉仪,并基于测量的参数来计算热声参数。使用超声波检查右旋糖酐水溶液的物理化学行为的应用包括理解分子相互作用的性质。研究了浓度和温度对右旋糖酐水溶液热声特性的影响。氢键、电荷转移络合物以及氢键和络合物的溶解只是分子之间存在的力以及分析如何解释其性质的几个例子。存在微弱的分子间作用力。超声波技术的最新发展使其成为评估液体分子物理和化学行为信息的有效工具。
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引用次数: 0
Our Contribution to Microwave-Assisted Conversions of Bioactive Compounds 我们对微波辅助生物活性化合物转化的贡献
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-06-09 DOI: 10.2174/2213335610666230609121927
B. Das, Nayaki Salva Reddy, A. Rathod, S. Avula, R. Das
The microwave chemistry of several bioactive natural products and synthetic compounds was studied by us. The compounds of different types, such as alkaloid, terpenoid, lignan, etc. were considered for our investigation. Some indole compounds, as well as organosulfur and miscellaneous carbonyl compounds, were also included. The substrates were irradiated under microwave irradiation for a short time and the resulting products were characterized. The conversion was conducted without using any solvent. The catalysts were not required in many transformations, but in some cases, catalysts, mainly heterogeneous catalysts were needed. The experimental procedures were convenient, less expensive, and generally eco-friendly. The interesting results of our efforts are briefly discussed in the present article.
对几种具有生物活性的天然产物和合成化合物的微波化学进行了研究。我们考虑了不同类型的化合物,如生物碱、萜类、木脂素等。一些吲哚化合物,以及有机硫和杂羰基化合物,也包括在内。在微波短时间照射下,对所制备的基质进行了表征。在不使用溶剂的情况下进行了转化。在许多转化过程中不需要催化剂,但在某些情况下需要催化剂,主要是多相催化剂。实验过程方便,便宜,而且通常是环保的。本文简要地讨论了我们努力的有趣结果。
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引用次数: 1
Effect of microwave radiation on the solvent-free synthesis of phthaloylamino acids 微波辐射对无溶剂合成邻苯二甲酸的影响
IF 0.8 Q4 CHEMISTRY, MULTIDISCIPLINARY Pub Date : 2023-05-23 DOI: 10.2174/2213335610666230523114340
N. Pankrushina, M. O. Korotkikh, A. N. Mikheev
In recent years, microwave radiation has been widely used in organic synthesis, including solvent-free mode. However, the reaction conditions of phthalic anhydride with amino acids under solvent-free microwave activation have not been studied so far.In the present work, the effect of microwave activation on the interaction of phthalic anhydride with amino acids in solvent-free conditions has been studied in detail.The microwave heating dynamics of phthalic anhydride, glycine and their equimolar mixture under microwave conditions have been investigated, and the dependence of the heating rate on the microwave power is defined.The common conditions for the synthesis of phthaloylamino acids have been determined as continuous heating at a power of 200 W at 130 °C for 5-6 min and additional heating for 5-10 min at a temperature close to the melting point of the corresponding amino acid. We apply the developed two-step solvent-free microwave reaction protocol successfully for the synthesis of phthaloyl derivatives of glycine, alanine, β-alanine, 4-aminobenzoic acid, γ-aminobutyric acid, isoleucine, leucine, phenylalanine.Reaction conditions for synthesizing phthaloylamino acids by microwave activation without solvent have been established. The solvent-free microwave reaction between phthalic anhydride and amino acid has been found to proceed in the melted phthalic anhydride.
近年来,微波辐射已广泛应用于有机合成,包括无溶剂模式。但目前对邻苯二酸酐与氨基酸在无溶剂微波活化下的反应条件还没有研究。本文详细研究了微波活化对邻苯二酸酐与氨基酸在无溶剂条件下相互作用的影响。研究了邻苯二酸酐、甘氨酸及其等摩尔混合物在微波条件下的微波加热动力学,确定了加热速率与微波功率的关系。合成邻苯二甲酰氨基酸的常用条件是在130°C下以200 W的功率连续加热5-6分钟,并在接近相应氨基酸熔点的温度下额外加热5-10分钟。我们成功地应用开发的两步无溶剂微波反应方案合成了甘氨酸、丙氨酸、β-丙氨酸、4-氨基苯甲酸、γ-氨基丁酸、异亮氨酸、亮氨酸、苯丙氨酸的邻苯甲酰衍生物。建立了无溶剂微波活化法合成邻苯二甲酸的反应条件。发现邻苯二酸酐与氨基酸在熔融的邻苯二酸酐中发生无溶剂微波反应。
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引用次数: 0
期刊
Current Microwave Chemistry
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