Journal ArticleDOI
Fluorine in Medicinal Chemistry
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TLDR
A tutorial review of fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency is provided in this paper. But the authors do not discuss the role of substitution.Abstract:
It has become evident that fluorinated compounds have a remarkable record in medicinal chemistry and will play a continuing role in providing lead compounds for therapeutic applications. This tutorial review provides a sampling of renowned fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency.read more
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The Medicinal Chemist's Toolbox: An Analysis of Reactions Used in the Pursuit of Drug Candidates
TL;DR: The reaction types used in the pursuit of novel drug candidates are analyzed to evaluate their frequency of occurrence, alongside other factors such as drug likeness, chirality, and the number of steps to each derivative.
Journal ArticleDOI
Catalysis for fluorination and trifluoromethylation
TL;DR: Reactions to make organofluorides that have emerged within the past few years are discussed and which exemplify how to overcome some of the intricate challenges associated with fluorination.
Journal ArticleDOI
The merger of transition metal and photocatalysis
TL;DR: The combination of Photoredox catalysis and transition metal catalysis is reviewed to show how this provides access to highly reactive oxidation states of transition metals and distinct activation modes that further enable the synthetic chemist.
Journal ArticleDOI
Trifluoromethylation of arenes and heteroarenes by means of photoredox catalysis
TL;DR: A mild, operationally simple strategy for the direct trifluoromethylation of unactivated arenes and heteroarenes through a radical-mediated mechanism using commercial photocatalysts and a household light bulb is reported.
Journal ArticleDOI
Organic synthesis provides opportunities to transform drug discovery
David C. Blakemore,Luis Castro,Ian Churcher,David C. Rees,Andrew Thomas,David Matthew Wilson,Anthony Wood +6 more
TL;DR: This Perspective highlights some of the most pressing challenges to be overcome from the industrial viewpoint — such as the development of reactions tolerating specific functionalities — and encourages stronger industry–academia relationships.
References
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Journal ArticleDOI
Fluorine in medicinal chemistry.
TL;DR: This tutorial review provides a sampling of renowned fluorinated drugs and their mode of action with a discussion clarifying the role and impact of fluorine substitution on drug potency.