Recent advances in cyclization reactions of isatins or thioisatins via C-N or C-S bond cleavage

2021 ◽  
Author(s):  
Jinhui Shen ◽  
Lei Zhang ◽  
Xiangtai Meng
Keyword(s):  
Medicinal Chemistry ◽  
Raw Materials ◽  
Bond Cleavage ◽  
Synthetic Methods ◽  
Cyclization Reactions ◽  
Recent Advances ◽  
Efficient Construction

The exploration of new reactivity modes and synthetic methods has always been an attractive goal of organic and medicinal chemistry. As potential raw materials for the efficient construction of nitrogen-...

scholarly journals Recent Advances in Catalytic Synthesis of Benzosultams

Molecules ◽  
2020 ◽  
Vol 25 (19) ◽  
pp. 4367
Author(s):  
Quan-Qing Zhao ◽  
Xiao-Qiang Hu
Keyword(s):  
Medicinal Chemistry ◽  
Catalytic Synthesis ◽  
Chiral Catalysts ◽  
Catalytic Systems ◽  
The Past ◽  
Recent Advances ◽  
Efficient Construction

Benzosultams represent one category of multi-heteroatom heterocyclic scaffolds, which have been frequently found in pharmaceuticals, agricultural agents, and chiral catalysts. Given the diversely significant functions of these compounds in organic and medicinal chemistry, great efforts have been made to develop novel catalytic systems for the efficient construction of benzosultam motifs over the past decades. Herein, in this review, we mainly summarize the recent advances in the field of catalytic synthesis of benzosultams from 2017 to August of 2020, with an emphasis on the scopes and mechanisms of representative reactions.

scholarly journals Recent Advances in the Synthetic Biology of Natural Drugs

2021 ◽  
Vol 9 ◽  
Author(s):  
Chun-Qiang Li ◽  
Hong-Mei Lei ◽  
Qian-Yi Hu ◽  
Guo-Hong Li ◽  
Pei-Ji Zhao
Keyword(s):  
Synthetic Biology ◽  
Large Scale ◽  
Raw Materials ◽  
Pharmaceutical Products ◽  
Synthetic Methods ◽  
Present Review ◽  
Plant Metabolites ◽  
Advantages And Disadvantages ◽  
Recent Advances ◽  
Natural Drugs

Natural drugs have been transformed and optimized during the long process of evolution. These compounds play a very important role in the protection of human health and treatment of human diseases. Sustainable approaches to the generation of raw materials for pharmaceutical products have been extensively investigated in drug research and development because chemical synthesis is costly and generates pollution. The present review provides an overview of the recent advances in the synthetic biology of natural drugs. Particular attention is paid to the investigations of drugs that may be mass-produced by the pharmaceutical industry after optimization of the corresponding synthetic systems. The present review describes the reconstruction and optimization of biosynthetic pathways for nine drugs, including seven drugs from plant sources and two drugs from microbial sources, suggesting a new strategy for the large-scale preparation of some rare natural plant metabolites and highly bioactive microbial compounds. Some of the suggested synthetic methods remain in a preliminary exploration stage; however, a number of these methods demonstrated considerable application potential. The authors also discuss the advantages and disadvantages of the application of synthetic biology and various expression systems for heterologous expression of natural drugs. Thus, the present review provides a useful perspective for researchers attempting to use synthetic biology to produce natural drugs.

Transition-Metal-Catalyzed Alkylation of Polyfluoroarenes through C–F Bond Cleavage

Synlett ◽  
2021 ◽  
Author(s):  
Tao Xiong ◽  
Qian Zhang ◽  
Qian Zhang
Keyword(s):  
Transition Metal ◽  
Medicinal Chemistry ◽  
Materials Science ◽  
Bond Cleavage ◽  
Recent Advances ◽  
Transition Metal Catalyzed ◽  
Metal Catalyzed ◽  
Site Selective

AbstractThe polyfluoroarenes are a subgroup of organofluorines that are widely utilized in both medicinal chemistry and materials science. We briefly summarize recent advances in the synthesis of these important compounds, with particular attention to our recent CuH-catalyzed defluorinative alkylation of polyfluoroarenes with alkenes in a highly site-selective C–F bond-cleavage fashion.1 Introduction2 Transition-Metal-Catalyzed Alkylation through Selective C–F Bond Cleavage3 CuH-Catalyzed Defluorinative Alkylation of Polyfluoroarenes with Alkenes4 Summary and Outlook

scholarly journals Recent Advances in the Synthesis of Piperazines: Focus on C–H Functionalization

Organics ◽  
2021 ◽  
Vol 2 (4) ◽  
pp. 337-347
Author(s):  
Carolina Durand ◽  
Michal Szostak
Keyword(s):  
Drug Discovery ◽  
Medicinal Chemistry ◽  
Structural Diversity ◽  
Synthetic Methods ◽  
Nitrogen Heterocycle ◽  
Piperazine Ring ◽  
The Third ◽  
Recent Advances ◽  
Made In

Piperazine ranks as the third most common nitrogen heterocycle in drug discovery, and it is the key component of several blockbuster drugs, such as Imatinib (also marketed as Gleevec) or Sildenafil, sold as Viagra. Despite its wide use in medicinal chemistry, the structural diversity of piperazines is limited, with about 80% of piperazine-containing drugs containing substituents only at the nitrogen positions. Recently, major advances have been made in the C–H functionalization of the carbon atoms of the piperazine ring. Herein, we present an overview of the recent synthetic methods to afford functionalized piperazines with a focus on C–H functionalization.

scholarly journals Recent Advances in the Development of Sigma Receptor Ligands as Cytotoxic Agents: A Medicinal Chemistry Perspective

2021 ◽  
Author(s):  
Antonino N. Fallica ◽  
Valeria Pittalà ◽  
Maria N. Modica ◽  
Loredana Salerno ◽  
Giuseppe Romeo ◽  
...  
Keyword(s):  
Medicinal Chemistry ◽  
Cytotoxic Agents ◽  
Sigma Receptor ◽  
Receptor Ligands ◽  
Sigma Receptor Ligands ◽  
Recent Advances

Recent advances for handling imbalancement and uncertainty in labelling in medicinal chemistry data analysis

2016 ◽  
Author(s):  
Joao Carlos Silva de Souza ◽  
Suzana Gomes Claudino ◽  
Rodolfo da Silva Simoes ◽  
Patricia Rufino Oliveira ◽  
Kathia Maria Honorio
Keyword(s):  
Data Analysis ◽  
Medicinal Chemistry ◽  
Chemistry Data ◽  
Recent Advances

scholarly journals New cyclization reactions in organic syntheses

2002 ◽  
Vol 74 (1) ◽  
pp. 159-166 ◽  
Author(s):  
Iwao Ojima
Keyword(s):  
Amino Acids ◽  
Transition Metal ◽  
Total Synthesis ◽  
Cyclization Reactions ◽  
Organic Syntheses ◽  
Carbocyclic Compounds ◽  
Efficient Construction ◽  
Transition Metal Catalyzed ◽  
Metal Catalyzed

Recent development in the transition metal-catalyzed cyclization reactions for organic syntheses in the author's laboratories is summarized, which includes (i) novel silylcarbocyclizations (SiCaCs) and carbonylative carbotricyclizations, (ii) intramolecular silylformylations and desymmerization of siloxydiynes by sequential double silylformylation, (iii) efficient total synthesis of (+)-prosopinine, (iv) enantioselective desymmetrization of aminodienes, and (iv) new and efficient routes to 1-azabicyclo[x.y.0]alkane amino acids. All these processes are catalyzed by Rh or Rh­Co complexes, and useful for rapid and efficient construction of a variety of heterocyclic and carbocyclic compounds. Mechanisms of these new carbocyclization and cyclohydrocarbonylation reactions are also discussed.

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