operational simplicity
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2022 ◽  
Vol 8 (1) ◽  
pp. 10
Author(s):  
Ozgun Civelekoglu ◽  
A. Bruno Frazier ◽  
A. Fatih Sarioglu

The magnetic separation of cells based on certain traits has a wide range of applications in microbiology, immunology, oncology, and hematology. Compared to bulk separation, performing magnetophoresis at micro scale presents advantages such as precise control of the environment, larger magnetic gradients in miniaturized dimensions, operational simplicity, system portability, high-throughput analysis, and lower costs. Since the first integration of magnetophoresis and microfluidics, many different approaches have been proposed to magnetically separate cells from suspensions at the micro scale. This review paper aims to provide an overview of the origins of microfluidic devices for magnetic cell separation and the recent technologies and applications grouped by the targeted cell types. For each application, exemplary experimental methods and results are discussed.


Synthesis ◽  
2022 ◽  
Author(s):  
Yu Tang ◽  
Biao Yu

A mild heteroatom methylation protocol using trimethyl phosphate (TMP)-Ca(OH)2 combination has been developed, which proceeds in DMF, or water, or under neat conditions at 80 oC or at room temperature. A series of O-, N- and S-nucleophiles, including phenols, sulfonamides, N-heterocycles such as 9H-carbazole, indole derivatives, 1,8-naphthalimide, and aryl/alkyl thiols are suitable substrates of this protocol. The high efficiency, operational simplicity, scalability, cost-efficiency, and environmental friendly nature of this protocol make it an attractive alternative to the conventional base prompted heteroatom methylation procedures.


2021 ◽  
Author(s):  
Shi-Chao Ren ◽  
Xing Yang ◽  
Bivas Mondal ◽  
Chengli Mou ◽  
Weiyi Tian ◽  
...  

Abstract The carbene and photocatalyst co-catalyzed radical coupling of acyl electrophile and a radical precursor is emerging as attractive method for ketone synthesis. However, previous reports mainly limited to prefunctionalized radical precursors and two-component coupling. Herein, an N-heterocyclic carbene and photocatalyst catalyzed decarboxylative radical coupling of carboxylic acids and acyl imidazoles is disclosed, in which the carboxylic acids were directly used as radical precursors. The acyl imidazoles could also be generated in situ by reaction of a carboxylic acid with CDI thus furnishing a formally decarboxylative coupling of two carboxylic acids. In addition, the reaction was successfully extended to three-component coupling by using alkene as a third coupling partner via a radical relay process. The mild conditions, operational simplicity, and use of carboxylic acids as the reacting partners make our method a powerful strategy for construction of complex ketones from readily available starting materials, and late-stage modification of natural products and medicines.


2021 ◽  
Vol 12 (1) ◽  
Author(s):  
Diandra S. Hassan ◽  
Christian Wolf

AbstractThe advances of high-throughput experimentation technology and chemometrics have revolutionized the pace of scientific progress and enabled previously inconceivable discoveries, in particular when used in tandem. Here we show that the combination of chirality sensing based on small-molecule optical probes that bind to amines and amino alcohols via dynamic covalent or click chemistries and powerful chemometric tools that achieve orthogonal data fusion and spectral deconvolution yields a streamlined multi-modal sensing protocol that allows analysis of the absolute configuration, enantiomeric composition and concentration of structurally analogous—and therefore particularly challenging—chiral target compounds without laborious and time-consuming physical separation. The practicality, high accuracy, and speed of this approach are demonstrated with complicated quaternary and octonary mixtures of varying chemical and chiral compositions. The advantages over chiral chromatography and other classical methods include operational simplicity, increased speed, reduced waste production, low cost, and compatibility with multiwell plate technology if high-throughput analysis of hundreds of samples is desired.


Synlett ◽  
2021 ◽  
Author(s):  
Gaochen Xu ◽  
Huan Yan ◽  
Sai Zhang ◽  
Qinghuan Wu ◽  
Jindian Duan ◽  
...  

A new method of FeCl2-catalyzed [4 + 2] annulation of α,β-unsaturated ketoxime acetates with N-acetyl enamides in batch and flow is reported. The current strategy features low-cost catalytic system, use of electron-rich olefins, operational simplicity and broad substrate scope, thus providing a facile and efficient access to substituted pyridines in moderate to good yields.


Antioxidants ◽  
2021 ◽  
Vol 10 (9) ◽  
pp. 1462
Author(s):  
Daniela Maria Biondi ◽  
Claudia Sanfilippo ◽  
Angela Patti

Limonene is one of the most abundant naturally occurring cyclic monoterpenes and has recently emerged as a sustainable alternative to petroleum-based solvents as well as a chemical platform for the production of value-added compounds. The biocatalytic epoxidation of both enantiomers of limonene was carried out in the presence of a peroxygenase-containing preparation from oat (Avena sativa) flour. Different reaction profiles were observed depending on the starting enantiomer of limonene, but in both cases the 1,2-monoepoxide was obtained as the main product with excellent diastereoselectivity. Trans-1,2-monoepoxide and cis-1,2-monoepoxide were isolated from the reaction of (R)-limonene and (S)-limonene, respectively, and the reactions were scaled-up to 0.17 M substrate concentration. The process is valuable for operational simplicity, lack of toxic metal catalysts, and cost-effectiveness of the enzymatic source. Pure stereoisomers of 1,2-monoepoxides of limonene constitute a useful starting material for biorenewable polymers, but can be also converted into other chiral derivatives by epoxide ring opening with nucleophiles. As a proof of concept, a tandem protocol for the preparation of enantiopure (1S,2S,4R)-1,2-diol from (R)-limonene and (1R,2R,4S)-1,2-diol from (S)-limonene was developed.


2021 ◽  
Author(s):  
Song Lin ◽  
Luiz Novaes ◽  
Justin Ho ◽  
Kaining Mao ◽  
Kaida Liu ◽  
...  

The “magic methyl” effect – a dramatic boost in the potency of biologically active compounds from the incorporation of a single methyl group – provides a simple yet powerful strategy employed by medicinal chemists in the drug discovery process. Despite significant advances, methodologies that enable the selective C(sp3)–H methylation of structurally complex medicinal agents remain very limited. In this work, we disclose a modular, efficient, and selective strategy for the α-methylation of protected amines (i.e., amides, carbamates, and sulfonamides) by means of electrochemical oxidation. Mechanistic analysis guided our development of an improved electrochemical protocol on the basis of the classic Shono oxidation reaction, which features broad reaction scope, high functional group compatibility, and operational simplicity. Importantly, this reaction system is amenable to the late-stage functionalization of complex targets containing basic nitrogen groups that are prevalent in medicinally active agents. When combined with organozinc-mediated C–C bond formation, our protocol enabled the direct methylation of a myriad of amine derivatives including those that have previously been explored for the “magic methyl” effect. This synthetic strategy thus circumvents multistep de novo synthesis that is currently necessary to access such compounds and has the potential to accelerate drug discovery efforts.


2021 ◽  
Author(s):  
Song Lin ◽  
Luiz Novaes ◽  
Justin Ho ◽  
Kaining Mao ◽  
Kaida Liu ◽  
...  

The “magic methyl” effect – a dramatic boost in the potency of biologically active compounds from the incorporation of a single methyl group – provides a simple yet powerful strategy employed by medicinal chemists in the drug discovery process. Despite significant advances, methodologies that enable the selective C(sp3)–H methylation of structurally complex medicinal agents remain very limited. In this work, we disclose a modular, efficient, and selective strategy for the α-methylation of protected amines (i.e., amides, carbamates, and sulfonamides) by means of electrochemical oxidation. Mechanistic analysis guided our development of an improved electrochemical protocol on the basis of the classic Shono oxidation reaction, which features broad reaction scope, high functional group compatibility, and operational simplicity. Importantly, this reaction system is amenable to the late-stage functionalization of complex targets containing basic nitrogen groups that are prevalent in medicinally active agents. When combined with organozinc-mediated C–C bond formation, our protocol enabled the direct methylation of a myriad of amine derivatives including those that have previously been explored for the “magic methyl” effect. This synthetic strategy thus circumvents multistep de novo synthesis that is currently necessary to access such compounds and has the potential to accelerate drug discovery efforts.


2021 ◽  
Vol 7 (9) ◽  
pp. 121
Author(s):  
Hyo-Yeon Yu ◽  
Sangki Myoung ◽  
Sangdoo Ahn

Benchtop nuclear magnetic resonance (NMR) spectroscopy uses small permanent magnets to generate magnetic fields and therefore offers the advantages of operational simplicity and reasonable cost, presenting a viable alternative to high-field NMR spectroscopy. In particular, the use of benchtop NMR spectroscopy for rapid in-field analysis, e.g., for quality control or forensic science purposes, has attracted considerable attention. As benchtop NMR spectrometers are sufficiently compact to be operated in a fume hood, they can be efficiently used for real-time reaction and process monitoring. This review introduces the recent applications of benchtop NMR spectroscopy in diverse fields, including food science, pharmaceuticals, process and reaction monitoring, metabolomics, and polymer materials.


Synthesis ◽  
2021 ◽  
Author(s):  
Goutam Brahmachari ◽  
Mullicka Mandal ◽  
Indrajit Karmakar

AbstractThe present communication deals with a straightforward, efficient, and green synthesis of a series of racemic version of 3-[3-(2-hydroxyphenyl)-3-oxo-1-arylpropyl]-4-hydroxycoumarins as biologically interesting warfarin analogues upon decarboxylative hydrolysis of bis-coumarin derivatives in aqueous potassium hydroxide solution. The salient features of this practical method are operational simplicity, avoidance of any organic solvents and tedious column chromatographic purification, clean reaction profiles, excellent yields, and gram-scale synthetic applicability.


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