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Artificial macrocycles recently became popular as a novel research field in drug discovery. As opposed to their natural twins, artificial macrocycles promise to have better control on synthesizability and control over their physicochemical properties resulting in druglike properties. Very few synthetic methods allow for the convergent, fast but diverse
Abdelraheem +3 more
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Symmetric Macrocycles by a Prins Dimerization and Macrocyclization Strategy [PDF]
A tandem dimerization/macrocyclization reaction utilizing the Prins cyclization has been developed. This reaction develops molecular complexity through the formation of highly substituted dimeric tetrahydropyran macrocycles. Mild conditions utilizing rhenium(VII) catalysts were explored for aromatic substrates, while harsher Lewis acidic conditions ...
Michael R, Gesinski +2 more
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Macrocyclic Drugs and Synthetic Methodologies toward Macrocycles [PDF]
Macrocyclic scaffolds are commonly found in bioactive natural products and pharmaceutical molecules. So far, a large number of macrocyclic natural products have been isolated and synthesized. The construction of macrocycles is generally considered as a crucial and challenging step in the synthesis of macrocyclic natural products.
Xufen Yu, Dianqing Sun
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Citation: 'macrocycle' in the IUPAC Compendium of Chemical Terminology, 3rd ed.; International Union of Pure and Applied Chemistry; 2006. Online version 3.0.1, 2019. 10.1351/goldbook.M03662 • License: The IUPAC Gold Book is licensed under Creative Commons Attribution-ShareAlike CC BY-SA 4.0 International for individual terms.
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Macrocycles are an emerging and largely underexploited part of chemical space where potential drugs for difficult genomic targets can be discovered. Macrocycles can have advantages over their natural twins such as better control over synthesis, physicochemical properties and target binding.
Abdelraheem, Eman M.M. +2 more
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Integrating Kinetics into Synthetic Studies via Adaptable Concentration-Dependent Yield Analysis. [PDF]
Xiao X +4 more
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Cross-dehydrogenative coupling macrocyclization for the construction of donor-acceptor nanohoops. [PDF]
Chakraborty B +4 more
europepmc +1 more source
The Convergent Synthetic Efforts toward Knightol and a Simplified Analog. [PDF]
Jeremia L +3 more
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