scholarly journals Rhodium-catalyzed, P-directed selective C7 arylation of indoles

2018 ◽  
Vol 4 (12) ◽  
pp. eaau6468 ◽  
Author(s):  
Xiaodong Qiu ◽  
Hong Deng ◽  
Yue Zhao ◽  
Zhuangzhi Shi
Keyword(s):  
Present Method ◽  
Rational Design ◽  
High Selectivity ◽  
Vital Role ◽  
Direct Arylation ◽  
Formal Synthesis ◽  
Marine Alkaloid ◽  
Aryl Bromides ◽  
Directing Group ◽  
Selection Of

The indole scaffold will continue to play a vital role in the future of drug discovery and agrochemical development. Regioselective direct arylation of indoles on the benzenoid moiety is a challenging task due to the inherent reactivity of the C2 and C3 positions. Here, we have developed an effective strategy for the regioselective direct arylation of indoles at the C7 position with (hetero)aryl bromides by the rational design of a directing group. The key to the high selectivity and reactivity of this method is the appropriate selection of a class of directing groups, N-PR2(R =tBu andcHex), that are easily removed in the presence of the Wilkinson’s catalyst. Using the present method as a key step, formal synthesis of marine alkaloid dictyodendrin B has also been demonstrated.

Selective photoredox direct arylations of aryl bromides in water in a microfluidic reactor

2021 ◽  
Vol 19 (13) ◽  
pp. 3016-3023
Author(s):  
Francesca Pallini ◽  
Elena Sangalli ◽  
Mauro Sassi ◽  
Philippe M. C. Roth ◽  
Sara Mattiello ◽  
...  
Keyword(s):  
High Selectivity ◽  
High Efficiency ◽  
Direct Arylation ◽  
Microfluidic Reactor ◽  
Aryl Bromides ◽  
Microflow Reactor

Performing photoredox direct arylation reactions under emulsion conditions in a microflow reactor enables high efficiency and high selectivity thanks to the favorable compartmentalization of the reagents and reactants.

Energy Efficiency Analysis in ERA using NFL-BA Algorithm

2020 ◽  
pp. 340-348
Author(s):  
Palky Mehta ◽  
H. L. Sharma
Keyword(s):  
Cluster Head ◽  
Vital Role ◽  
Wireless Sensor ◽  
Energy Usage ◽  
Cluster Heads ◽  
Comparison Results ◽  
Current Scenario ◽  
Energy Efficiency Analysis ◽  
Selection Of

In the current scenario of Wireless Sensor Network (WSN), power consumption is the major issue associated with nodes in WSN. LEACH technique plays a vital role of clustering in WSN and reduces the energy usage effectively. But LEACH has its own limitation in order to search cluster head nodes which are randomly distributed over the network. In this paper, ERA-NFL- BA algorithm is being proposed for selects the cluster heads in WSN. This algorithm help in selection of cluster heads can freely transform from global search to local search. At the end, a comparison has been done with earlier researcher using protocol ERA-NFL, which clearly shown that proposed Algorithm is best suited and from comparison results that ERA-NFL-BA has given better performance.

Selection of high-quality sperm with thousands of parallel channels

Lab on a Chip ◽  
2021 ◽  
Author(s):  
Mohammad Simchi ◽  
Jason Riordon ◽  
Jae Bem You ◽  
Yihe Wang ◽  
Sa Xiao ◽  
...  
Keyword(s):  
Clinical Practice ◽  
High Selectivity ◽  
High Yield ◽  
Sperm Selection ◽  
High Quality ◽  
Parallel Channels ◽  
Selection Of

A 3D-structured sperm selection device is presented that achieves both high selectivity and high yield via thousands of parallel channels. The device significantly outperforms the best clinical practice by selecting ∼100 000 of higher-quality sperm.

Direct Arylation of Heteroaromatic Compounds with Congested, Functionalised Aryl Bromides at Low Palladium/Triphosphane Catalyst Loading

2011 ◽  
Vol 17 (23) ◽  
pp. 6453-6461 ◽  
Author(s):  
David Roy ◽  
Sophal Mom ◽  
Dominique Lucas ◽  
Hélène Cattey ◽  
Jean‐Cyrille Hierso ◽  
...  
Keyword(s):  
Catalyst Loading ◽  
Direct Arylation ◽  
Heteroaromatic Compounds ◽  
Aryl Bromides

Recent Progress on Apoptotic Activity of Triazoles

2021 ◽  
Vol 22 ◽  
Author(s):  
Pelin Çıkla-Süzgün ◽  
Ş. Güniz Küçükgüzel
Keyword(s):  
Cancer Progression ◽  
Anticancer Agents ◽  
Heterocyclic Compounds ◽  
Rational Design ◽  
Vital Role ◽  
Anticancer Activities ◽  
The Past ◽  
Small Molecule Drugs ◽  
Apoptotic Activity ◽  
New Generation

Abstract: Apoptosis, often called programmed cell death, is a self-directed cell destruction process. It differs from classical necrosis by activation of caspases. Apoptosis is directly related to cancer progression and plays a vital role in carcinogenesis. All cytotoxic drugs and radiation therapy programs initiates apoptosis in tumor cells. Today, studies show that heterocyclic compounds that contain triazole funtionality have anticancer activities. Triazoles are 5-membered rings, which contain two carbon and three nitrogen atoms Therefore, many researchers have synthesized these small active compounds as target structures and evaluated their apoptotic activities. The present review describs more recent medicinal aspects of triazoles as anticancer agents reported during the past few years. We hope that the bioactivity of triazole derivatives will be beneficial for the rational design of new generation of small molecule drugs.

Automation Tool Preparation in the Conditions of Production

2015 ◽  
Vol 770 ◽  
pp. 739-743 ◽  
Author(s):  
A.S. Yuanyushkin ◽  
D.V. Lobanov ◽  
D.A. Rychkov
Keyword(s):  
Comparative Analysis ◽  
Rational Design ◽  
Economic Effect ◽  
Optimal Choice ◽  
Processing Efficiency ◽  
Time Required ◽  
The Given ◽  
High Processing ◽  
Selection Of

The key task of the tool manufacturing is to create or to choose such a type of tool, which would permit to provide high processing efficiency, the best tool`s workability and the quality of the machined surfaces with minimum expenses and resources. The optimal choice of the constructive tool modifications from a variety of options takes much time required for the preparation of the tool to work. To solve this problem, we have developed software that allows you to create, organize and carry out a comparative analysis of structural instruments in order to identify rational option for the given conditions of production. Ordering and selection of a rational design of the instrument is carried out in accordance with established procedures of modeling and comparative analysis of design solutions. Application software can reduce design time technological process by 80...90%, and get a substantial annual economic effect.

scholarly journals Quinoxaline as an integrated directing group in palladium-catalyzed ortho-C–H bond arylation of the aryl unit of 2-arylquinoxalines

2018 ◽  
Vol 42 (19) ◽  
pp. 16036-16039 ◽  
Author(s):  
Imane Idris ◽  
Fazia Derridj ◽  
Thierry Roisnel ◽  
Henri Doucet ◽  
Jean-François Soulé
Keyword(s):  
Aryl Bromides ◽  
Palladium Catalyzed ◽  
Directing Group

ortho-Directed arylation of the C(sp2)–H bond of 2-arylquinoxalines with a broad range of aryl bromides was achieved using phosphine-free Pd(OAc)2.

Particle Swarm Optimization Based Algorithm for Ship Vertical Passage Layout Optimization

2012 ◽  
Vol 479-481 ◽  
pp. 1885-1888
Author(s):  
Wen Quan Wang ◽  
Sheng Huang ◽  
Yu Long Hu ◽  
Yuan Hang Hou
Keyword(s):  
Particle Swarm Optimization ◽  
Rational Design ◽  
Particle Swarm Optimization Algorithm ◽  
Particle Swarm ◽  
Vital Role ◽  
Layout Problem ◽  
Swarm Optimization ◽  
Operation And Maintenance ◽  
Simulation Results ◽  
The Mathematical Model

The passage plays a vital role in operation and maintenance of naval ships. The rational design of the passage could increase the efficiency of combat logistics, life-cycle logistics and personnel movement under combat and emergency conditions. Borrowing ideas from facility layout, the model of optimal vertical passage layout was established to formulation the vertical passage layout problem. The Floyd’s algorithm was used to calculate the distance between two compartments and the particle swarm optimization algorithm was proposed to solve the mathematical model. From simulation results, the model and methods are feasible for the vertical passage layout problem.

Sign in / Sign up

Export Citation Format

Share Document