Synthetic Approaches to Tetracyclic Indolines as Versatile Building Blocks of Diverse Indole Alkaloids

2018 ◽  
Vol 24 (54) ◽  
pp. 14302-14315 ◽  
Author(s):  
Yanshi Wang ◽  
Fukai Xie ◽  
Bin Lin ◽  
Maosheng Cheng ◽  
Yongxiang Liu
Keyword(s):  
Indole Alkaloids ◽  
Building Blocks ◽  
Synthetic Approaches

Synthesis and Biological Potentials of Quinoline Analogues: A Review of Literature

2019 ◽  
Vol 16 (7) ◽  
pp. 653-688 ◽  
Author(s):  
Leena Kumari ◽  
Salahuddin ◽  
Avijit Mazumder ◽  
Daman Pandey ◽  
Mohammad Shahar Yar ◽  
...  
Keyword(s):  
Biological Activity ◽  
Heterocyclic Compounds ◽  
Building Blocks ◽  
Vital Role ◽  
Review Of Literature ◽  
Drug Discovery Process ◽  
Active Compounds ◽  
Lead Compounds ◽  
Synthetic Approaches ◽  
Derivatives Of

Heterocyclic compounds are well known for their different biological activity. The heterocyclic analogs are the building blocks for synthesis of the pharmaceutical active compounds in the organic chemistry. These derivatives show various type of biological activity like anticancer, antiinflammatory, anti-microbial, anti-convulsant, anti-malarial, anti-hypertensive, etc. From the last decade research showed that the quinoline analogs plays a vital role in the development of newer medicinal active compounds for treating various type of disease. Quinoline reported for their antiviral, anticancer, anti-microbial and anti-inflammatory activity. This review will summarize the various synthetic approaches for synthesis of quinoline derivatives and to check their biological activity. Derivatives of quinoline moiety plays very important role in the development of various types of newer drugs and it can be used as lead compounds for future investigation in the field of drug discovery process.

scholarly journals Borylation and rearrangement of alkynyloxiranes: a stereospecific route to substituted α-enynes

2019 ◽  
Vol 15 ◽  
pp. 1416-1424
Author(s):  
Ruben Pomar Fuentespina ◽  
José Angel Garcia de la Cruz ◽  
Gabriel Durin ◽  
Victor Mamane ◽  
Jean-Marc Weibel ◽  
...  
Keyword(s):  
Organic Synthesis ◽  
Cross Coupling ◽  
Functional Materials ◽  
Building Blocks ◽  
Cascade Process ◽  
Coupling Reactions ◽  
One Pot ◽  
Bioactive Natural Products ◽  
Cross Coupling Reactions ◽  
Synthetic Approaches

1,3-Enynes are important building blocks in organic synthesis and also constitute the key motif in various bioactive natural products and functional materials. However, synthetic approaches to stereodefined substituted 1,3-enynes remain a challenge, as they are limited to Wittig and cross-coupling reactions. Herein, stereodefined 1,3-enynes, including tetrasubstituted ones, were straightforwardly synthesized from cis or trans-alkynylated oxiranes in good to excellent yields by a one-pot cascade process. The procedure relies on oxirane deprotonation, borylation and a stereospecific rearrangement of the so-formed alkynyloxiranyl borates. This stereospecific process overall transfers the cis or trans-stereochemistry of the starting alkynyloxiranes to the resulting 1,3-enynes.

Recent developments in the synthesis of azaindoles from pyridine and pyrrole building blocks

2021 ◽  
Author(s):  
Damoder Reddy Motati ◽  
Radhika Amaradhi ◽  
Thota Ganesh
Keyword(s):  
Natural Products ◽  
Building Blocks ◽  
Bioactive Natural Products ◽  
Biological Importance ◽  
Recent Developments ◽  
Synthetic Approaches

The azaindole framework is ubiquitous in bioactive natural products and pharmaceuticals. This review highlights the synthetic approaches to azaindoles with advantages and limitations, mechanistic pathways and biological importance.

ChemInform Abstract: Building Blocks for the Synthesis of Indole Alkaloids: Stereoselective Protonation of Butyrolactone Enolate.

ChemInform ◽  
1990 ◽  
Vol 21 (2) ◽  
Author(s):  
D. SPITZNER ◽  
K. ARNOLD ◽  
J. J. STEZOWSKI ◽  
T. HILDENBRAND ◽  
S. HENKEL
Keyword(s):  
Indole Alkaloids ◽  
Building Blocks

Efficient Synthetic Approaches to the Common Scaffold of Indole Alkaloids

2007 ◽  
Vol 9 (20) ◽  
pp. 3913-3916 ◽  
Author(s):  
Redouane Beniazza ◽  
Julie Dunet ◽  
Frédéric Robert ◽  
Kurt Schenk ◽  
Yannick Landais
Keyword(s):  
Indole Alkaloids ◽  
The Common ◽  
Synthetic Approaches

Synthetic Approaches to Contemporary Drugs that Contain the Cyclopropyl Moiety

Synthesis ◽  
2020 ◽  
Vol 52 (09) ◽  
pp. 1315-1345 ◽  
Author(s):  
Zdenko Časar
Keyword(s):  
Drug Administration ◽  
Structural Diversity ◽  
Building Blocks ◽  
Time Frame ◽  
New Drugs ◽  
Diazo Compounds ◽  
Structural Motif ◽  
Ch Acids ◽  
Synthetic Approaches ◽  
The U.S

The U.S. Food and Drug Administration approved 18 new drugs that incorporate the cyclopropyl structural motif in the time frame from 2012 to 2018. This review provides an overview of synthetic approaches to these drugs with emphasis on the construction of the cyclopropyl moiety or its incorporation into the key building blocks for assembly of the highlighted drugs. Based on the structural diversity of these drugs, synthetic approaches for the construction and introduction of the cyclopropyl moiety into their structure are diverse and include: cycloalkylation (double alkylation) of CH-acids, catalytic cyclopropanation of alkenes with diazo compounds, the Simmons–Smith reaction, the Corey–Chaykovsky reaction, the Kulinkovich reaction, the Horner–Wadsworth–Emmons reaction, and cycloaddition. In addition, the cyclopropyl structure was also introduced into the drug substance intermediates via simple cyclopropyl-moiety-containing building blocks, such as cyclopropylamine, cyclopropanesulfonamide, cyclopropanecarbonyl chloride, and cyclopropylmagnesium bromide.1 Introduction2 Synthesis of Recently Approved Cyclopropyl-Moiety-Containing Drugs2.1 Cabozantinib2.2 Trametinib2.3 Simeprevir2.4 Ledipasvir2.5 Olaparib2.6 Tasimelteon2.7 Finafloxacin2.8 Paritaprevir2.9 Lenvatinib2.10 Lumacaftor2.11 Lesinurad2.12 Grazoprevir2.13 Glecaprevir2.14 Ozenoxacin2.15 Voxilaprevir2.16 Naldemedine2.17 Tezacaftor2.18 Tecovirimat3 Conclusion

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