Journal ArticleDOI
Analysis of the Structural Diversity, Substitution Patterns, and Frequency of Nitrogen Heterocycles among U.S. FDA Approved Pharmaceuticals
TLDR
This review reports on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals, and reports detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.Abstract:
Nitrogen heterocycles are among the most significant structural components of pharmaceuticals. Analysis of our database of U.S. FDA approved drugs reveals that 59% of unique small-molecule drugs contain a nitrogen heterocycle. In this review we report on the top 25 most commonly utilized nitrogen heterocycles found in pharmaceuticals. The main part of our analysis is divided into seven sections: (1) three- and four-membered heterocycles, (2) five-, (3) six-, and (4) seven- and eight-membered heterocycles, as well as (5) fused, (6) bridged bicyclic, and (7) macrocyclic nitrogen heterocycles. Each section reveals the top nitrogen heterocyclic structures and their relative impact for that ring type. For the most commonly used nitrogen heterocycles, we report detailed substitution patterns, highlight common architectural cores, and discuss unusual or rare structures.read more
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Photoredox Catalysis in Organic Chemistry
TL;DR: This Perspective highlights the unique ability of photoredox catalysis to expedite the development of completely new reaction mechanisms, with particular emphasis placed on multicatalytic strategies that enable the construction of challenging carbon-carbon and carbon-heteroatom bonds.
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Applications of Palladium-Catalyzed C–N Cross-Coupling Reactions
TL;DR: An overview of Pd-catalyzed N-arylation reactions found in both basic and applied chemical research from 2008 to the present is provided.
Journal ArticleDOI
3d Transition Metals for C-H Activation.
Parthasarathy Gandeepan,Thomas Müller,Daniel Zell,Gianpiero Cera,Svenja Warratz,Lutz Ackermann +5 more
TL;DR: A comprehensive overview on first row transition metal catalysts for C-H activation until summer 2018 is provided.
Journal ArticleDOI
The medicinal chemist's toolbox for late stage functionalization of drug-like molecules
TL;DR: This review details a toolbox of intermolecular C-H functionalization chemistries with proven applicability to drug-like molecules, classified by regioselectivity patterns, and gives guidance on how to systematically develop LSF strategies using these patterns and other considerations.
Journal ArticleDOI
Contribution of Organofluorine Compounds to Pharmaceuticals.
TL;DR: This mini-review analyzes the prevalence of fluoro-pharmaceuticals in the market and categorizes them into several groups based on the chemotype of thefluoro-functional groups, their therapeutic purpose, and the presence of heterocycles and/or chirality to highlight the structural motifs, patterns, and promising trends in fluorine-based drug design.
References
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Irwin Goldstein,Tom F. Lue,Harin Padma-Nathan,Raymond C. Rosen,William D. Steers,Pierre A. Wicker +5 more
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Marine indole alkaloids: potential new drug leads for the control of depression and anxiety
TL;DR: Information is provided on current and potential pharmaceuticals including small molecule natural indole alkaloids to their biological properties, structure-activity relationship studies, and especially their potential for the treatment of neurological disorders, including depression.
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Rings in Drugs
TL;DR: Analysis of rings, ring systems, and frameworks in drugs listed in the FDA Orange Book gives insight into the chemical novelty of drugs and potentially efficient ways to assess compound libraries and develop compounds from hit identification to lead optimization and beyond.
Journal ArticleDOI
Data-mining for sulfur and fluorine: an evaluation of pharmaceuticals to reveal opportunities for drug design and discovery.
TL;DR: The evolution and structural diversity of sulfur and the popular integration of fluorine into drugs introduced over the past 50 years are evaluated and promoted to promote innovative insights into drug development.
Journal ArticleDOI
Metallodrugs in Medicinal Inorganic Chemistry
Katja Dralle Mjos,Chris Orvig +1 more