Synthesis of Privileged Scaffolds by Using Diversity-Oriented Synthesis

2013 ◽  
Vol 8 (6) ◽  
pp. 1168-1176 ◽  
Author(s):  
Ramu Surakanti ◽  
Sumalatha Sanivarapu ◽  
Chiranjeevi Thulluri ◽  
Pravin S. Iyer ◽  
Raghuram S. Tangirala ◽  
...  
Keyword(s):  
Diversity Oriented Synthesis ◽  
Privileged Scaffolds

Flow synthesis approaches to privileged scaffolds – recent routes reviewed for green and sustainable aspects

2021 ◽  
Vol 23 (6) ◽  
pp. 2233-2292
Author(s):  
Antonella Ilenia Alfano ◽  
Margherita Brindisi ◽  
Heiko Lange
Keyword(s):  
Green Chemistry ◽  
Flow Chemistry ◽  
Diversity Oriented Synthesis ◽  
Flow Synthesis ◽  
Versatile Tool ◽  
Privileged Scaffolds

This review discusses the use of flow chemistry as versatile tool for the synthesis and derivatisation of privileged scaffolds, looking at applicability, diversity-oriented synthesis options, inherent sustainability and green chemistry aspects.

Corrigendum: Synthesis of Privileged Scaffolds by Using Diversity-Oriented Synthesis

2014 ◽  
Vol 9 (7) ◽  
pp. 1706-1706
Author(s):  
Ramu Surakanti ◽  
Sumalatha Sanivarapu ◽  
Chiranjeevi Thulluri ◽  
Pravin S. Iyer ◽  
Raghuram S. Tangirala ◽  
...  
Keyword(s):  
Diversity Oriented Synthesis ◽  
Privileged Scaffolds

Cascade CuH-Catalyzed Conversion of Alkynes to Enantioenriched 1,1-Disubstituted Products

2019 ◽  
Author(s):  
De-Wei Gao ◽  
Yang Gao ◽  
Huiling Shao ◽  
Tian-Zhang Qiao ◽  
Xin Wang ◽  
...  
Keyword(s):  
Organic Synthesis ◽  
Medicinal Chemistry ◽  
Proteasome Inhibitors ◽  
Building Blocks ◽  
Unique Role ◽  
Efficient Strategy ◽  
Carbon Centers ◽  
Rapid Access ◽  
Cascade Catalysis ◽  
Privileged Scaffolds

Enantioenriched <i>α</i>-aminoboronic acids play a unique role in medicinal chemistry and have emerged as privileged pharmacophores in proteasome inhibitors. Additionally, they represent synthetically useful chiral building blocks in organic synthesis. Recently, CuH-catalyzed asymmetric alkene hydrofunctionalization has become a powerful tool to construct stereogenic carbon centers. In contrast, applying CuH cascade catalysis to achieve reductive 1,1-difunctionalization of alkynes remains an important, but largely unaddressed, synthetic challenge. Herein, we report an efficient strategy to synthesize <i>α</i>-aminoboronates <i>via </i>CuH-catalyzed hydroboration/hydroamination cascade of readily available alkynes. Notably, this transformation selectively delivers the desired 1,1-heterodifunctionalized product in favor of alternative homodifunctionalized, 1,2-heterodifunctionalized, or reductively monofunctionalized byproducts, thereby offering rapid access to these privileged scaffolds with high chemo-, regio- and enantioselectivity.<br>

Formation of Carbon-Oxygen Bond Mediated by Hypervalent Iodine Reagents Under Metal-free Conditions

2020 ◽  
Vol 17 ◽  
Author(s):  
Ayesha Jalil ◽  
Yaxin O Yang ◽  
Zhendong Chen ◽  
Rongxuan Jia ◽  
Tianhao Bi ◽  
...  
Keyword(s):  
Natural Products ◽  
Bond Formation ◽  
Building Blocks ◽  
Review Article ◽  
Hypervalent Iodine ◽  
Metal Free ◽  
Bioactive Natural Products ◽  
The Past ◽  
Oxygen Bond ◽  
Privileged Scaffolds

: Hypervalent iodine reagents are a class of non-metallic oxidants have been widely used in the construction of several sorts of bond formations. This surging interest in hypervalent iodine reagents is essentially due to their very useful oxidizing properties, combined with their benign environmental character and commercial availability from the past few decades ago. Furthermore, these hypervalent iodine reagents have been used in the construction of many significant building blocks and privileged scaffolds of bioactive natural products. The purpose of writing this review article is to explore all the transformations in which carbon-oxygen bond formation occurred by using hypervalent iodine reagents under metal-free conditions

Diversity-oriented synthesis of polymer membranes with ion solvation cages

Nature ◽  
2021 ◽  
Vol 592 (7853) ◽  
pp. 225-231
Author(s):  
Miranda J. Baran ◽  
Mark E. Carrington ◽  
Swagat Sahu ◽  
Artem Baskin ◽  
Junhua Song ◽  
...  
Keyword(s):  
Polymer Membranes ◽  
Ion Solvation ◽  
Diversity Oriented Synthesis

scholarly journals Diversity-oriented synthesis derived indole based spiro and fused small molecules kills artemisinin-resistant Plasmodium falciparum

2021 ◽  
Vol 20 (1) ◽  
Author(s):  
Akshaykumar Nayak ◽  
Himani Saxena ◽  
Chandramohan Bathula ◽  
Tarkeshwar Kumar ◽  
Souvik Bhattacharjee ◽  
...  
Keyword(s):  
Plasmodium Falciparum ◽  
Small Molecules ◽  
New Drugs ◽  
Developmental Cycle ◽  
Oxygen Species ◽  
Compound Library ◽  
Diversity Oriented Synthesis ◽  
Resistant Strains ◽  
Acid Catalyzed

Abstract Background Despite numerous efforts to eradicate the disease, malaria continues to remain one of the most dangerous infectious diseases plaguing the world. In the absence of any effective vaccines and with emerging drug resistance in the parasite against the majority of anti-malarial drugs, the search for new drugs is urgently needed for effective malaria treatment. Methods The goal of the present study was to examine the compound library, based on indoles generated through diversity-oriented synthesis belonging to four different architecture, i.e., 1-aryltetrahydro/dihydro-β-carbolines and piperidine/pyrrolidine-fused indole derivatives, for their in vitro anti-plasmodial activity. Trifluoroacetic acid catalyzed transformation involving tryptamine and various aldehydes/ketones provided the library. Results Among all the compounds screened, 1-aryltetrahydro-β-carbolines 2 and 3 displayed significant anti-plasmodial activity against both the artemisinin-sensitive and artemisinin-resistant strain of Plasmodium falciparum. It was observed that these compounds inhibited the overall parasite growth in intra-erythrocytic developmental cycle (IDC) via reactive oxygen species-mediated parasitic death and thus could be potential anti-malarial compounds. Conclusion Overall the compounds 2 and 3 identified in this study shows promising anti-plasmodial activity that can kill both artemisinin-sensitive and artemisinin-resistant strains of P. falciparum.

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