‘Wake-Up Call of A Sleeping Beauty’: Straightforward Synthesis of Functionalized β-(2-Pyridyl) Ketones from 2,6-Lutidine

Synlett ◽  
2017 ◽  
Vol 28 (10) ◽  
pp. 1219-1223 ◽  
Author(s):  
Laure Bouchez ◽  
Cyril Gerbeaux ◽  
Marion Rusch ◽  
Maude Patoor ◽  
Madeleine Livendahl ◽  
...  
Keyword(s):  
Natural Products ◽  
Physicochemical Properties ◽  
Building Block ◽  
Sleeping Beauty ◽  
Starting Material ◽  
Step Process ◽  
Small Set ◽  
One Step ◽  
The Common

β-(2-Pyridyl) ketones are a unique class of heterocycles with valuable physicochemical properties and emerging relevance as pharmacophores. Herein we report a one-step process for the preparation of various substituted β-(2-pyridyl) ketones from the common starting material, 2,6-lutidine. Furthermore, we demonstrate the utility of this building block by synthesizing of a small set of antimalarial natural products.

Rapid Plasma-Assisted, Ambient-Pressure Deposition of Conformal Nanocrystalline Zinc Oxide Thin Films for Solar Cell Applications

2011 ◽  
Vol 1323 ◽  
Author(s):  
Joachim D. Pedersen ◽  
Kwok Siong Teh
Keyword(s):  
Deposition Temperature ◽  
Ambient Pressure ◽  
Zno Thin Film ◽  
Step Process ◽  
Fused Quartz ◽  
One Step ◽  
The Common ◽  
Deposited Films ◽  
Nanocrystalline Zinc Oxide ◽  
Made In

ABSTRACTThis paper reports a plasma-assisted, rapid, ambient-pressure, low-temperature one-step process for depositing conformal, non-porous nanocrystalline ZnO thin film on various substrates ranging from Si (100), fused quartz, glass, muscovite, c- and a-plane sapphire (Al2O3), to the common polymer polyimide (KaptonTM). The as-synthesized polycrystalline films range in thickness from 20nm to 200nm, deposited at a growth rate ranging from 2 nm/min to 50 nm/min. The lowest deposition temperature achieved with this method is 180°C and progress is being made in further lowering this temperature. The as-deposited films are highly oriented in the caxis, with (002) being the dominant planes.

Residual Gas Reactions in the Electron Microscope: IV. A Factor in Radiation Damage

1971 ◽  
Vol 29 ◽  
pp. 74-75
Author(s):  
Richard E. Hartman ◽  
Roberta S. Hartman
Keyword(s):  
Electron Microscope ◽  
Inelastic Scattering ◽  
Radiation Damage ◽  
Common Assumption ◽  
Step Process ◽  
One Step ◽  
The Common ◽  
Residual Gas ◽  
Gas Reactions ◽  
Dose Dependent

The common assumption that in the electron microscope there is a minimum, irreducible, dose-dependent damage to the specimen caused by inelastic scattering of electrons implies that such damage results from a one - step process. We now have evidence that this assumption is open to serious question.

Direct Cyclization of Alkenyl Thioester via Transition Metal‐hydrogen Atom Transfer/radical‐polar Crossover Mechanism

2019 ◽  
Author(s):  
Shiori Date ◽  
Kensei Hamasaki ◽  
Karen Sunagawa ◽  
Hiroki Koyama ◽  
Chikayoshi Sebe ◽  
...  
Keyword(s):  
Natural Products ◽  
Hydrogen Atom ◽  
Transition Metal ◽  
Hydrogen Atom Transfer ◽  
Synthetic Method ◽  
Atom Transfer ◽  
Reaction Conditions ◽  
Hydride Hydrogen ◽  
Sulfur Heterocycles ◽  
One Step

<div>We report here a catalytic, Markovnikov selective, and scalable synthetic method for the synthesis of saturated sulfur heterocycles, which are found in the structures of pharmaceuticals and natural products, in one step from an alkenyl thioester. Unlike a potentially labile alkenyl thiol, an alkenyl thioester is stable and easy to prepare. The powerful Co catalysis via a cobalt hydride hydrogen atom transfer and radical-polar crossover mechanism enabled simultaneous cyclization and deprotection. The substrate scope was expanded by the extensive optimization of the reaction conditions and tuning of the thioester unit.</div>

One-step Separation and Purification of Four Phenolic Acids from Stenoloma chusanum (L.) Ching by Medium-pressure Liquid Chromatography and High-speed Counter-current Chromatography

2019 ◽  
Vol 9 (2) ◽  
pp. 138-143
Author(s):  
Tianyun Li ◽  
Xiling Dai ◽  
Yichen Li ◽  
Guozheng Huang ◽  
Jianguo Cao
Keyword(s):  
Natural Products ◽  
Liquid Chromatography ◽  
Phenolic Acids ◽  
High Speed ◽  
High Efficiency ◽  
Total Phenolic ◽  
Medium Pressure ◽  
Medium Pressure Liquid Chromatography ◽  
One Step ◽  
Counter Current

Background:Stenoloma chusanum (L.) Ching is a Chinese traditional medicinal fern with high total flavonoid and total phenolic content. Traditionally, phenolic compounds were separated by using column chromatography, which is relatively inefficient. </P><P> Objective: This study aims to use an efficient method to separate natural products from S. chusanum by Medium-Pressure Liquid Chromatography (MPLC) and High-Speed Counter-Current Chromatography (HSCCC).Methods:In the present research, firstly, a sample (2.5 g) from the dichloromethane extract of S. chusanum was separated by MPLC. Next, fraction P5 was purified by HSCCC with a two-phase solvent system composed of hexane-ethyl acetate-methanol-water (HEMWat) at a volume ratio of 2:4:1:4 (v/v/v/v). </P><P> Result: Four phenolic acids were obtained and their structures were identified by means of NMR and ESI-mass analysis. They were identified as: 1) protocatechuic acid (34 mg, purity 90.1%), 2) syringic acid (66 mg, purity 99.0%), 3) p-hydroxybenzoic acid (5 mg, purity 91.2%) and 4) vanillic acid (6 mg, purity 99.3%).Conclusion:The combination of MPLC and HSCCC is a high-efficiency separation method for natural products. This is the first report with regard to the separation of four phenolic acids in one step by MPLC and HSCCC from S. chusanum (L.) Ching.

Formal Total Syntheses of Crocacin A-D

2005 ◽  
Vol 70 (10) ◽  
pp. 1696-1708 ◽  
Author(s):  
Magnus Besev ◽  
Christof Brehm ◽  
Alois Fürstner
Keyword(s):  
Natural Products ◽  
Aldol Reaction ◽  
Cross Coupling ◽  
Coupling Reactions ◽  
Total Syntheses ◽  
Cross Coupling Reactions ◽  
Palladium Catalyzed ◽  
The Common ◽  
Selective Addition

A concise route to the common polyketide fragment5of crocacin A-D (1-4) is presented which has previously been converted into all members of this fungicidal and cytotoxic family of dipeptidic natural products by various means. Our synthesis features asyn-selective titanium aldol reaction controlled by a valinol-derived auxiliary, a zinc-mediated, palladium-catalyzedanti-selective addition of propargyl mesylate10to the chiral aldehyde9, as well as a comparison of palladium-catalyzed Stille and Suzuki cross-coupling reactions for the formation of the diene moiety of the target.

Synthesis of Polycycles and Oxacycles by Tandem Metathesis of endo–norbornene Derivatives

Synthesis ◽  
2021 ◽  
Author(s):  
Sambasivarao Kotha ◽  
Sunil Pulletikurti ◽  
Ambareen Fatma ◽  
gopal dhangar ◽  
gonna somu Naidu
Keyword(s):  
Natural Products ◽  
Metal Complex ◽  
Carbonyl Group ◽  
Single Step ◽  
Time Dependent ◽  
Computational Studies ◽  
Nmr Studies ◽  
Tricyclic Compounds ◽  
One Step ◽  
Norbornene Derivatives

Here, we have demonstrated that the presence of a carbonyl group at C7 position is preventing the olefin metathesis of endo-norbornene derivatives due to the complexation of the metal alkylidene. Time-dependent NMR studies showed the presence of new proton signals in the metal alkylidene region, which indicate the formation of metal complex with the carbonyl group of the substrate. These observations were further proved by ESI-MS analysis. Whereas, computational studies provided that the catalyst was interacting with the C7 carbonyl group and aligned perpendicular to that of norbornene olefin. Later, these endo-keto norbornene derivatives were reduced to hydroxyl derivatives diastereoselectively. Ring-rearrangement metathesis (RRM) of these hydroxyl derivatives, produced the [6/5/6], and [5/6/5] carbo-tricyclic cores of the natural products in one step. Whereas the RRM of O-allyl derivatives, delivered the oxa-tricyclic compounds in a single step with excellent yields.

scholarly journals Is Dialdehyde Chitosan a Good Substance to Modify Physicochemical Properties of Biopolymeric Materials?

2021 ◽  
Vol 22 (7) ◽  
pp. 3391
Author(s):  
Sylwia Grabska-Zielińska ◽  
Alina Sionkowska ◽  
Ewa Olewnik-Kruszkowska ◽  
Katarzyna Reczyńska ◽  
Elżbieta Pamuła
Keyword(s):  
Mechanical Properties ◽  
Tissue Engineering ◽  
Physicochemical Properties ◽  
Silk Fibroin ◽  
Three Dimensional ◽  
Microscopy Imaging ◽  
Maximum Deformation ◽  
One Step ◽  
Chitosan Blends ◽  
Fourier Transfer Infrared Spectroscopy

The aim of this work was to compare physicochemical properties of three dimensional scaffolds based on silk fibroin, collagen and chitosan blends, cross-linked with dialdehyde starch (DAS) and dialdehyde chitosan (DAC). DAS was commercially available, while DAC was obtained by one-step synthesis. Structure and physicochemical properties of the materials were characterized using Fourier transfer infrared spectroscopy with attenuated total reflectance device (FTIR-ATR), swelling behavior and water content measurements, porosity and density observations, scanning electron microscopy imaging (SEM), mechanical properties evaluation and thermogravimetric analysis. Metabolic activity with AlamarBlue assay and live/dead fluorescence staining were performed to evaluate the cytocompatibility of the obtained materials with MG-63 osteoblast-like cells. The results showed that the properties of the scaffolds based on silk fibroin, collagen and chitosan can be modified by chemical cross-linking with DAS and DAC. It was found that DAS and DAC have different influence on the properties of biopolymeric scaffolds. Materials cross-linked with DAS were characterized by higher swelling ability (~4000% for DAS cross-linked materials; ~2500% for DAC cross-linked materials), they had lower density (Coll/CTS/30SF scaffold cross-linked with DAS: 21.8 ± 2.4 g/cm3; cross-linked with DAC: 14.6 ± 0.7 g/cm3) and lower mechanical properties (maximum deformation for DAC cross-linked scaffolds was about 69%; for DAS cross-linked scaffolds it was in the range of 12.67 ± 1.51% and 19.83 ± 1.30%) in comparison to materials cross-linked with DAC. Additionally, scaffolds cross-linked with DAS exhibited higher biocompatibility than those cross-linked with DAC. However, the obtained results showed that both types of scaffolds can provide the support required in regenerative medicine and tissue engineering. The scaffolds presented in the present work can be potentially used in bone tissue engineering to facilitate healing of small bone defects.

A chemoinformatic analysis of atoms, scaffolds and functional groups in natural products

2021 ◽  
Vol 0 (0) ◽  
Author(s):  
Joelle Ngo Hanna ◽  
Boris D. Bekono ◽  
Luc C. O. Owono ◽  
Flavien A. A. Toze ◽  
James A. Mbah ◽  
...  
Keyword(s):  
Natural Products ◽  
Drug Discovery ◽  
Physicochemical Properties ◽  
Functional Groups ◽  
Atomic Composition ◽  
Synthetic Compounds ◽  
Chemical Libraries ◽  
Synthetic Drugs ◽  
Drugs Analysis ◽  
Chemical Class

Abstract In the quest to know why natural products (NPs) have often been considered as privileged scaffolds for drug discovery purposes, many investigations into the differences between NPs and synthetic compounds have been carried out. Several attempts to answer this question have led to the investigation of the atomic composition, scaffolds and functional groups (FGs) of NPs, in comparison with synthetic drugs analysis. This chapter briefly describes an atomic enumeration method for chemical libraries that has been applied for the analysis of NP libraries, followed by a description of the main differences between NPs of marine and terrestrial origin in terms of their general physicochemical properties, most common scaffolds and “drug-likeness” properties. The last parts of the work describe an analysis of scaffolds and FGs common in NP libraries, focusing on huge NP databases, e.g. those in the Dictionary of Natural Products (DNP), NPs from cyanobacteria and the largest chemical class of NP – terpenoids.

Synthetic Strategies to Access Heteroatomic Spirocentres Embedded in Natural Products

Synthesis ◽  
2021 ◽  
Author(s):  
Michael P. Badart ◽  
Bill C. Hawkins
Keyword(s):  
Natural Products ◽  
Heterocyclic Compound ◽  
Chemical Space ◽  
Three Dimensional ◽  
Coupling Reactions ◽  
Conjugate Additions ◽  
Biological Targets ◽  
Compound Libraries ◽  
The Common ◽  
Significant Attention

AbstractThe spirocyclic motif is abundant in natural products and provides an ideal three-dimensional template to interact with biological targets. With significant attention historically expended on the synthesis of flat-heterocyclic compound libraries, methods to access the less-explored three-dimensional medicinal-chemical space will continue to increase in demand. Herein, we highlight by reaction class the common strategies used to construct the spirocyclic centres embedded in a series of well-studied natural products.1 Introduction2 Cycloadditions3 Palladium-Catalysed Coupling Reactions4 Conjugate Additions5 Imines, Aminals, and Hemiaminal Ethers6 Mannich-Type Reactions7 Oxidative Dearomatisation8 Alkylation9 Organometallic Additions10 Conclusions

Functionalized aluminum-catalyzed silicon nanowire formation and radial junction photovoltaic devices

Nanoscale ◽  
2021 ◽  
Author(s):  
Wipakorn Jevasuwan ◽  
Naoki Fukata
Keyword(s):  
Surface Modification ◽  
Solar Cells ◽  
Surface Defects ◽  
Silicon Nanowire ◽  
Photovoltaic Devices ◽  
Step Process ◽  
One Step ◽  
Length Reduction

Vertical Al-catalyzed SiNW arrays with shaped surfaces were synthesized by a one-step process and NW-based solar cells were demonstrated with optimized NW surface defects through surface modification and length reduction.

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