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Quantification of catalpol in root of Rehmannia glutinosa varieties 19 collected in Phu Tho province by high-performance liquid chromatography 用高效液相色谱法定量测定富都省采集的地黄 19 号品种根中的梓酚含量
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).20-24
Thanh Loan Pham
The active ingredient catalpol in the Rehmannia glutinosavariety 19 roots is an important chemical component. Catalpol has hypoglycemia, diuretic, and laxative effects; it is used to support the treatment of diabetes, ischemic cerebral, and dementia, and it is regulated by Vietnamese Pharmacopoeia V (2017) as a marker to check the quality of medicinal herbs. This study aimed to develop a procedure for quantifying catalpol in the root of Rehmannia glutinosa varieties 19 by high-performance liquid chromatography (HPLC) to evaluate the quality of medicinal herbs. The research results have selected suitable chromatographic conditions using the Gemini C18 column (250x4.6 mm, 5 μm), detector at 210 nm, mobile phase acetonitrile - phosphoric acid 0.1%, and flow rate at 0.6 ml/min. The peak area and catalpol concentration have a strong linear correlation with r=0.9999, Y = 21887X + 26213. The procedure has good accuracy and repeatability with a relative standard deviation (RSD) <2%. Quantitative results of catalpol in the root of the R. glutinosa varieties 19 reached 1.25%. The HPLC method is suitable for quantifying catalpol in the root of R. glutinosa varieties 19.
地黄 19 根中的有效成分梓酚是一种重要的化学成分。梓醇具有降血糖、利尿和通便的作用,可用于辅助治疗糖尿病、缺血性脑病和痴呆症,并被越南药典 V(2017 年)规定为检查药材质量的标志物。本研究旨在开发一种高效液相色谱法(HPLC)定量检测地黄 19 号品种根中梓醇含量的程序,以评估药材质量。研究结果选择了合适的色谱条件:Gemini C18色谱柱(250x4.6 mm,5 μm),检测波长为210 nm,流动相为乙腈-磷酸0.1%,流速为0.6 ml/min。峰面积与梓醇浓度呈较强的线性关系,r=0.9999,Y=21887X + 26213。该方法具有良好的准确性和重复性,相对标准偏差(RSD)小于 2%。糯稻品种 19 的根中梓醇的定量结果为 1.25%。该高效液相色谱法适用于定量检测 "芸苔素 19 "根中的梓酚含量。
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引用次数: 0
Morphology, anatomy, and quantitative determination of corosolic acid in Lagerstroemia calyculata Kurz in the Southeast region, Vietnam 越南东南地区 Lagerstroemia calyculata Kurz 的形态学、解剖学和科罗索酸的定量测定
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).25-30
Minh Tu To, Thi Xuyen Do, Thi Tuyet Hoang, Van Truong Phan, Minh Tu Dang, Thanh Huyen Pham
Objectives: To describe the morphological characteristics, anatomy (stem, leaves), and quantify the corosolic acid in the leaves of Lagerstroemia calyculata Kurz collected in the Southeast region, Vietnam. Subjects and methods: Using the comparative morphological method to determine the scientific name of species. Studying the microscopic characteristics of Lagerstroemia calyculataKurz according to the research method of N. Ba (2009) [1] and quantifying the content of corosolic acid in the leaves according to the United States Pharmacopeia 2017 (USP 40), with adjustments to suit the conditions of the laboratory. Results: Lagerstroemia calyculata Kurz is tree, deciduous, height 30-35 m, smooth bark. Leaves lanceolate, lateral veins 9-11 pairs, hairy. Inflorescence paniculate, small white flowers. Capsules ovoid, 6-valved. Seeds are numerous, brown, and smooth. The stem has a bicollateral vascular bundle, conduction tissue arranged continuously, double phloem pillars and leaf veins exposed on both sides. The outer epidermis has multicellular stellate hairs. Scattered in soft tissue there are crystalline particles. Stomata are present only on the underside of leaves. The quantification of corosolic acid in three leaf samples of Lagerstroemia calyculata Kurz was from 0.05 to 0.12%. Conclusions: This study has detailed morphological, anatomical characteristics, and quantitative determination of corosolic acid in three leaf samples of Lagerstroemia calyculata Kurz collected in the Southeast region.
研究目的描述在越南东南部地区采集的 Lagerstroemia calyculata Kurz 的形态特征、解剖结构(茎、叶),并量化叶片中的科罗索酸。研究对象和方法用形态比较法确定物种学名。根据 N. Ba(2009 年)[1] 的研究方法研究 Lagerstroemia calyculataKurz 的显微特征,并根据《美国药典 2017》(USP 40)对叶片中的科罗索酸含量进行定量,并根据实验室条件进行调整。结果Lagerstroemia calyculata Kurz 为乔木,落叶,高 30-35 米,树皮光滑。叶披针形,侧脉 9-11 对,有毛。花序圆锥状,小白花。蒴果卵球形,6瓣裂。种子多数,褐色,光滑。茎有双侧维管束,传导组织连续排列,双韧皮部支柱,叶脉两侧外露。外表皮有多细胞星状毛。软组织中散布着结晶颗粒。气孔只出现在叶片背面。在 Lagerstroemia calyculata Kurz 的三个叶片样本中,科罗索酸的定量为 0.05% 到 0.12%。研究结论本研究对在东南地区采集的三份 Lagerstroemia calyculata Kurz 叶片样本中的科罗索酸进行了详细的形态、解剖特征和定量测定。
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引用次数: 0
Application of solid-phase extraction materials from ion liquids for the analysis of carbamate pesticide 应用离子液体固相萃取材料分析氨基甲酸酯类农药
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).45-54
Van Duy Le, Thai The Nguyen, Hoang Phuong Tran, Anh Mai Nguyen
In this study, ionic liquid immobilised onto silica gel material SiO2-(CH2)3-N(Oct)3Br was successfully synthesised and characterised by Fourier-transform infrared spectroscopy (FT-IR), thermal gravimetric analysis (TGA), scanning electron microscopy (SEM), and energy-dispersive X-ray spectroscopy (EDX). This material was applied as the stationary phase of solid-phase extraction for the enrichment of trace amounts of carbamate pesticides in water. The cartridge was eluted with 5 ml of acetonitrile (ACN), blow-dried with nitrogen gas, and re-dissolved in ACN:H2O (40:60, v/v) and analysed by high-performance liquid chromatography - ultraviolet (HPLC-UV) at 210 and 245 nm. Within this process, elution of the cartridge with 5 ml of acetonitrile (ACN) was followed by nitrogen gas blow-drying and subsequent re-dissolution in ACN:H2O (40:60, v/v), culminating in analysis by HPLC-UV at 210 and 245 nm. Optimisation of conditions facilitated the analysis of carbamate pesticides, with the limit of quantitation (LOQ)ranging from 0.36-2.00 μg/l for tap water and 0.4-3.5 μg/l for river water. Furthermore, the method exhibited favourable repeatability, with a relative standard deviation (RSD) of less than 10%, thereby meeting the Association of Official Analytical Collaboration (AOAC) standards.
本研究成功合成了固定在硅胶材料 SiO2-(CH2)3-N(Oct)3Br 上的离子液体,并通过傅立叶变换红外光谱(FT-IR)、热重分析(TGA)、扫描电子显微镜(SEM)和能量色散 X 射线光谱(EDX)对其进行了表征。该材料被用作固相萃取的固定相,用于富集水中的痕量氨基甲酸酯类农药。用 5 毫升乙腈(ACN)洗脱滤芯,用氮气吹干,然后重新溶解在 ACN:H2O(40:60,v/v)中,并在 210 和 245 纳米波长下用高效液相色谱-紫外(HPLC-UV)进行分析。在此过程中,先用 5 毫升乙腈(ACN)洗脱滤芯,然后用氮气吹干,再重新溶解于 ACN:H2O(40:60,v/v)中,最后在 210 和 245 纳米波长下进行高效液相色谱-紫外分析。条件的优化有助于氨基甲酸酯类农药的分析,自来水的定量限(LOQ)为 0.36-2.00 μg/l,河水的定量限(LOQ)为 0.4-3.5 μg/l。此外,该方法的重复性良好,相对标准偏差(RSD)小于 10%,符合官方分析合作协会(AOAC)的标准。
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引用次数: 0
Prediction of geomechanical changes in faulted rock mass around underground structures subjected to earthquakes 预测受地震影响的地下结构周围断层岩体的地质力学变化
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).13-19
Q. Nguyen, Ngoc Hue Nguyen, Quang Minh Nguyen, V. Nguyen, Tuan Minh Tran
Faults are a type of geological structure that often leads to geological disasters in underground structures under normal conditions and especially when earthquakes occur, thereby requiring careful study.This article introduces some numerical simulation results on the seismic wave propagation process, on changes in stress and displacement states in the rock mass with a small fault of a dip angle of 45o, around a circular cross-section tunnel, using the discrete element method (Universal distinct element Code - UDEC). Three cases are simulated: a) The tunnel is located in the hanging wall rock, the fault is located 10m from the centre of the tunnel on the vertical axis; b) The fault runs through the centre of the tunnel and c) The tunnel is located in the footing wall rock, the fault is located 10m from the centre of the tunnel on the vertical axis. The results obtained show a very clear influence of the position and location of the fault on the geomechanical changes in the rock mass around the tunnel, contributing to the reasonable design of tunnels subjected to earthquakes.
断层是一种地质构造,在正常情况下,尤其是发生地震时,往往会导致地下结构发生地质灾害,因此需要对其进行仔细研究。本文采用离散元法(Universal distinct element Code - UDEC)介绍了地震波传播过程中的一些数值模拟结果,以及围绕圆形截面隧道的倾角为 45o 的小型断层岩体中应力和位移状态的变化。模拟了三种情况:a) 隧道位于悬壁岩中,断层位于纵轴上距隧道中心 10 米处;b) 断层穿过隧道中心;c) 隧道位于岩脚壁岩中,断层位于纵轴上距隧道中心 10 米处。所得结果表明,断层的位置和位置对隧道周围岩体的地质力学变化有非常明显的影响,有助于受地震影响的隧道的合理设计。
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引用次数: 0
Synthesis of TiO2 by hydrothermal method using deep eutectic solvent for application in dye-sensitised solar cell 利用深共晶溶剂通过水热法合成 TiO2,以应用于染料敏化太阳能电池
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).06-12
Doan Thanh Thuy Nguyen, De Nguyen, Huynh Trung Le Ly, Tuyet Phuong Nguyen
Raw TiO2 powder from a commercial source was used as a precursor in the hydrothermal process with deep eutectic solvent (DES) of choline chloride and urea with a molar ratio of 1:2 at different temperatures and interval times. The synthesised TiO2 was further utilised to produce diffracting TiO2 paste for application in dye-sensitised solar cells (DSCs) to improve the power conversation efficiency of devices. The TiO2 product analysed by X-ray diffraction (XRD) showed a similar phase and crystallinity to the raw material. However, scanning electron microscope (SEM) images showed that the hydrothermal TiO2 product had less particle aggregation than the raw one. The particle size was exceedingly 100 nm. The TiO2 pastes were prepared with a mixture of ethyl acetate and terpineol at volume ratios of 3:7 and 4:6. The paste was suitable to make thin films by the screen-printing method as a diffusion layer in cells. DSC devices using the TiO2 produced by the hydrothermal process with DES at 140oC for 18, 24, and 36 hours, respectively, enhanced the power conversion efficiency by 6.7-6.9%, which was higher than the ones using raw TiO2 by about 7%. Therefore, TiO2 powder modified by the hydrothermal process in DES solvent has great potential for application in DSC manufacture.
在不同温度和间隔时间下,以氯化胆碱和尿素的摩尔比为 1:2 的深共晶溶剂 (DES) 水热工艺中,使用商业来源的未加工二氧化钛粉末作为前体。合成的二氧化钛被进一步用于生产衍射二氧化钛浆料,以应用于染料敏化太阳能电池(DSCs),从而提高设备的功率转换效率。通过 X 射线衍射 (XRD) 分析的二氧化钛产品显示出与原材料相似的相位和结晶度。不过,扫描电子显微镜(SEM)图像显示,水热 TiO2 产品的颗粒聚集程度低于原材料。颗粒大小超过 100 纳米。二氧化钛浆料是用体积比为 3:7 和 4:6 的乙酸乙酯和松油醇混合物制备的。这种浆料适合用丝网印刷法制成薄膜,作为电池中的扩散层。使用水热法生产的 TiO2 与 DES 分别在 140oC 下加热 18、24 和 36 小时后,DSC 器件的功率转换效率提高了 6.7-6.9%,比使用未加工 TiO2 的器件高出约 7%。因此,在 DES 溶剂中通过水热法改性的 TiO2 粉末在 DSC 制造中具有巨大的应用潜力。
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引用次数: 0
Research and development of a predictive system for fall armyworm early warning on maize crop 研究和开发玉米作物秋季虫害预警预测系统
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).38-44
Thi Diep Hoang, Thi Anh Duong Nguyen, Kien Thai Duong Nguyen, Duy Vu Nguyen, Thi Quynh Trang Luu, Thi Thu Phuong Tran, Minh Trien Pham
The rapid increase in fall armyworms (FAW, Spodoptera frugiperda) in recent years has posed major challenges to maize growers around the globe. To keep larval density below the economic threshold, we need interdisciplinary agricultural solutions like plant protection epidemiology, the Internet of Things, and scientific data techniques for early detection, monitoring, forecasting, and making informed decisions. Pest control should be planned ahead of time to prevent indiscriminate pesticide spraying, waste, and a negative effect on the environment. In this study, the authors plan to create a comprehensive iFAWcast software system that will automatically predict, alert, and gather research data on fall armyworms on maize crops in Vietnam. The system is comprised of three major components: (i) An automatic forecasting and alerting tool for fall armyworm outbreaks on the web platform; (ii) An agriculture reporting, forecasting, alerting, and user management tool on the web platform; and (iii) A mobile app that provides forecasting and alerting services on fall armyworms to farmers based on their geographical location. The iFAWcast system includes a central computation that dynamically updates weather forecasts from the Visual Crossing API and the OpenWeatherMap API, as well as a formula for the effective cumulative temperature based on the characteristics of fall armyworms on maize crops in Vietnam. The developed system was tested using data collected straight from the field, yielding extremely accurate and dependable results.
近年来,秋绵虫(FAW,Spodoptera frugiperda)的迅速增加给全球玉米种植者带来了重大挑战。为了将幼虫密度控制在经济阈值以下,我们需要跨学科的农业解决方案,如植物保护流行病学、物联网和科学数据技术,以实现早期检测、监测、预测和做出明智决策。病虫害防治应提前规划,以防止农药滥喷、浪费和对环境造成负面影响。在本研究中,作者计划创建一个综合 iFAWcast 软件系统,该系统将自动预测、预警并收集越南玉米作物上秋季军虫的研究数据。该系统由三个主要部分组成:(i) 网络平台上的自动预报和警报工具;(ii) 网络平台上的农业报告、预报、警报和用户管理工具;(iii) 移动应用程序,根据农民的地理位置向他们提供有关秋虫的预报和警报服务。iFAWcast 系统包括一个中央计算,可动态更新来自 Visual Crossing API 和 OpenWeatherMap API 的天气预报,以及一个基于越南玉米作物上秋季军团虫特征的有效积温公式。使用直接从田间收集的数据对所开发的系统进行了测试,结果非常准确可靠。
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引用次数: 0
Development of NBS-LRR gene-specific microsatellite markers for passion fruit Passiflora edulis Sims 为西番莲开发 NBS-LRR 基因特异性微卫星标记
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).31-37
Duc Trung Tran, Thi Thu Hang Nguyen, Thu Huong Dao, Hong Linh Ta, Thi Lan Hoa Nguyen, Thanh Huyen Pham, Thi Hue Huong Tran, Hoang Nguyen
The chromosome-level genome assembly of passion fruit (Passiflora edulis Sims) has facilitated computational analyses in developing novel informative SSR markers for genetics and breeding research. In this study, in-silico analysis was conducted to discover potential microsatellite loci and to design specific primers from the sequences of the characterised nucleotide-binding site - leucine-rich repeats (NBS-LRR) gene family of passion fruit, and a genotyping experiment was performed to validate the novel simple sequence repeat (SSR) markers.In total, 497 microsatellite loci were detected from 161 passion fruit NBS-LRR genes, of which 383 loci were qualified for primer generation. Forty-six SSR markers were selected for polymorphism verification, targeting 35 NBS-LRR genes that showed potential gene expression in response to biotic and abiotic stresses. From that, 25 SSR markers showed consistent polymorphic alleles among different passion fruit genotypes via PCR-PAGE analysis. These novel NBS-LRR-specific SSR markers might provide valuable tools for fortifying research on germplasm evaluation, genetic mapping, and molecular breeding for disease-resistant passion fruit varieties.
百香果(Passiflora edulis Sims)染色体水平的基因组组装有助于进行计算分析,为遗传学和育种研究开发新的信息 SSR 标记。在这项研究中,研究人员从已鉴定的百香果核苷酸结合位点-富亮氨酸重复序列(NBS-LRR)基因家族的序列中,进行了发现潜在微卫星位点和设计特异性引物的海内分析,并进行了基因分型实验,以验证新型简单序列重复(SSR)标记。筛选出 46 个 SSR 标记进行多态性验证,目标是 35 个 NBS-LRR 基因,这些基因对生物和非生物胁迫有潜在的基因表达。通过 PCR-PAGE 分析,25 个 SSR 标记在不同百香果基因型中显示出一致的多态性等位基因。这些新型 NBS-LRR 特异性 SSR 标记可为加强抗病百香果品种的种质评估、基因图谱绘制和分子育种研究提供有价值的工具。
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引用次数: 0
Evolution of nuclear shell structure in neutron-rich nuclei N=32 and N=34 富中子核 N=32 和 N=34 的核壳结构演变
Pub Date : 2024-03-25 DOI: 10.31276/vjst.66(3).01-05
Cong Cuong Do, D. L. Bui, Duc Ton Nguyen
This paper presents an overview of the experimental setup to study the structure of unstable nuclear isotopes in the region from 47Cl to 63V of the SEASTAR 3 project and the evolution of shell structure in neutron-rich nuclei N=32 and N=34. The first excited energies of Cl, Ar, and K isotopes around N=32, N=34 obtained from the SEASTAR 3 project were determined. The evolution of shell structure in neutron-rich nuclei N=32 và N=34 is explained by the contribution of tensor forces in addition to central and spin-orbit forces. The appearance of new magic neutron N=34 in 54Ca is explained due to proton-neutron tensor force that pulls neutron 0f5/2 lower than 1p1/2 level, leading to not only causes the spin inversion of neutrons at 1p1/2 and 0f5/2 levels and enlarges an energy gap between these levels. The change of proton and neutron energy levels in Cl, Ar, and K isotopes around N=32, N=34 driven by tensor force was also discussed in this article.
本文概述了用于研究 SEASTAR 3 项目 47Cl 至 63V 区域不稳定核同位素结构的实验装置,以及富中子核 N=32 和 N=34 的壳结构演变。确定了 SEASTAR 3 项目获得的 N=32 和 N=34 附近 Cl、Ar 和 K 同位素的第一激发能量。除了中心力和自旋轨道力之外,张力的贡献也解释了富中子核 N=32 和 N=34 壳结构的演变。质子-中子张力将中子 0f5/2 拉低到 1p1/2 水平,不仅导致中子在 1p1/2 和 0f5/2 水平的自旋反转,而且扩大了这两个水平之间的能隙,从而解释了 54Ca 中新神奇中子 N=34 的出现。本文还讨论了在张力作用下,Cl、Ar 和 K 同位素中质子和中子能级在 N=32 和 N=34 附近的变化。
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引用次数: 0
Expression of several deubiquitinase and tyrosine phosphatase genes involved in inflammatory response in lymphoma 参与淋巴瘤炎症反应的几种去泛素酶和酪氨酸磷酸酶基因的表达
Pub Date : 2024-03-15 DOI: 10.31276/vjste.66(1).90-95
N. Giang, Nguyen Trong Ha, Nguyen Thi Xuan
Lymphoma represents a heterogeneous group of cancers affecting the lymphatic system, encompassing non-Hodgkin lymphoma (NHL) and Hodgkin lymphoma (HL). The majority of NHL cases originate from B cells. HL is characterized by the presence of rare Hodgkin and Reed-Sternberg cells. Within the context of the inflammatory response, two SH2 domain-containing protein tyrosine phosphatases (SHPs), namely SHP-1 and SHP-2, serve as negative regulators. Deubiquitinating enzymes (DUBs) play a crucial role in inhibiting NF-κB activation in response to various stimuli. This study focuses on the DUBs OTUB1, OTUB2, and Cezanne. Blood samples were collected from 50 NHL patients, 26 HL patients, and 50 healthy individuals. Quantitative RT-PCR was employed to assess the mRNA expression of OTUB1, OTUB2, Cezanne, SHP-1,and SHP-2, while ELISA was used to determine IL-6 and CA125 concentrations. The results revealed that the mRNA level of OTUB1 was significantly downregulated in NHL patients but not in HL patients. Notably, Cezanne expression was downregulated in lymphoma patients, with significantly lower levels observed in HL compared to NHL patients. Furthermore, SHP-1 mRNA expression was significantly lower in the NHL group compared to the HL group or healthy individuals. Conversely, SHP-2 gene expression was upregulated in NHL patients but remained unchanged in HL patients. In conclusion, these findings highlight significant differences in the expressions of DUB and SHP genes and the inflammatory response in lymphoma patients. This study provides a foundation for further investigation into the roles of DUBs and tyrosine phosphatases in regulating the functional activation of lymphoma cells.
淋巴瘤是影响淋巴系统的一组异质性癌症,包括非霍奇金淋巴瘤(NHL)和霍奇金淋巴瘤(HL)。大多数非霍奇金淋巴瘤源于 B 细胞。HL 的特点是存在罕见的霍奇金细胞和里德-斯特恩伯格细胞。在炎症反应的背景下,两种含 SH2 结构域的蛋白酪氨酸磷酸酶(SHPs),即 SHP-1 和 SHP-2 起着负调控作用。去泛素化酶(DUBs)在抑制 NF-κB 在各种刺激下的活化方面起着至关重要的作用。本研究的重点是 DUBs OTUB1、OTUB2 和 Cezanne。研究人员采集了 50 名 NHL 患者、26 名 HL 患者和 50 名健康人的血样。采用定量 RT-PCR 法评估 OTUB1、OTUB2、Cezanne、SHP-1 和 SHP-2 的 mRNA 表达,同时采用 ELISA 法测定 IL-6 和 CA125 的浓度。结果显示,OTUB1的mRNA水平在NHL患者中明显下调,而在HL患者中则没有。值得注意的是,Cezanne在淋巴瘤患者中表达下调,与NHL患者相比,HL患者的表达水平明显较低。此外,与HL组或健康人相比,NHL组的SHP-1 mRNA表达明显降低。相反,SHP-2 基因表达在 NHL 患者中上调,但在 HL 患者中保持不变。总之,这些发现突显了淋巴瘤患者中 DUB 和 SHP 基因表达及炎症反应的显著差异。这项研究为进一步研究 DUB 和酪氨酸磷酸酶在调节淋巴瘤细胞功能活化中的作用奠定了基础。
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引用次数: 0
Development of direct C-3 difluoromethylation reaction for application in synthesis of quinoline-related drugs 开发直接 C-3 二氟甲基化反应,用于合成喹啉相关药物
Pub Date : 2024-03-15 DOI: 10.31276/vjste.66(1).53-58
Thanh Tung Truong, John Nielsen
Fluorine holds a prominent position within the realm of drug discovery and development, substantiated by its presence in approximately 25% of drugs approved by the US Food and Drug Administration (FDA). Consequently, the advancement of new fluorination reactions stands as a pivotal area in medicinal chemistry. In particular, the monofluoro-, difluoromethyl-, and trifluoromethyl- are three groups that appear most frequently in drug structure. Quinoline, owing to its privileged structural status, plays a crucial role in drug design and synthesis. Various approaches have been documented for the direct difluoromethylation of the C-2 and C-4 positions of the quinoline ring. However, achieving direct C-3 difluoromethylation has remained an elusive objective. In this study, we introduce a novel method for effecting the direct difluoromethylation at the C-3 position of the quinoline ring.Comprehensive characterizations, including 1H-NMR, 13C-NMR, and 19F-NMR for all compounds are performed. We believe that this novel method will open a new way to access the hitherto untapped C-3-difluoromethylation active compounds.
氟在药物研发领域占有重要地位,美国食品药品管理局(FDA)批准的药物中约有 25% 含有氟。因此,推进新的氟化反应是药物化学的一个关键领域。其中,单氟、二氟甲基和三氟甲基是药物结构中出现频率最高的三个基团。喹啉因其特殊的结构地位,在药物设计和合成中起着至关重要的作用。目前已有多种方法可以直接对喹啉环的 C-2 和 C-4 位置进行二氟甲基化。然而,实现 C-3 直接二氟甲基化仍然是一个难以实现的目标。在本研究中,我们介绍了一种在喹啉环的 C-3 位实现直接二氟甲基化的新方法。我们对所有化合物进行了全面的表征,包括 1H-NMR、13C-NMR 和 19F-NMR。我们相信,这种新方法将为获得迄今尚未开发的 C-3-二氟甲基化活性化合物开辟一条新途径。
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引用次数: 0
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Ministry of Science and Technology, Vietnam
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