scispace - formally typeset
Journal ArticleDOI

Fluorinated Pyrazoles: From Synthesis to Applications.

TLDR
Analysis of novel synthetic approaches to fluorinated pyrazoles that appeared in recent years is performed, with a particular emphasis on a detailed consideration of reaction mechanisms.
Abstract
Fluorinated pyrazoles play an important role in medicinal chemistry, drug discovery, agrochemistry, coordination chemistry, and organometallic chemistry. Since the early 1990s, their popularity has grown exponentially. Moreover, more than 50% of all contributions on the topic have been published in the last 5 years. In this review, analysis of novel synthetic approaches to fluorinated pyrazoles that appeared in recent years is performed. A particular emphasis is devoted to a detailed consideration of reaction mechanisms. In addition, the reasons that have led to the ever-increasing popularity of fluorinated pyrazoles in various areas of science are discussed. At the end of the review, several potentially interesting but yet mostly unknown classes of fluorinated pyrazoles are outlined.

read more

Citations
More filters
Journal ArticleDOI

Copper-Catalyzed Cross-Coupling of Benzylic C-H Bonds and Azoles with Controlled N-Site Selectivity.

TL;DR: In this paper, a copper-catalyzed method was proposed to achieve site-selective cross-coupling of pyrazoles and other N-H heterocycles with substrates bearing (hetero)benzylic C-H bonds.
Journal ArticleDOI

Electro-oxidative C–H azolation of quinoxalin-2(1H)-ones

TL;DR: In this paper, the authors developed a practical, general protocol for direct C-H azolation reactions of quinoxalin-2(1H)-ones by electro-oxidative cross-coupling.
Journal ArticleDOI

Fluoroalkyl N-Triftosylhydrazones as Easily Decomposable Diazo Surrogates for Asymmetric [2 + 1] Cycloaddition: Synthesis of Chiral Fluoroalkyl Cyclopropenes and Cyclopropanes

TL;DR: The development of asymmetric carbene transfer reactions using N-sulfonylhydrazones as the diazo surrogate is a long-term issue in organic synthesis since N-Sulfon-hydrazone commonly require high computational complexity as discussed by the authors.
Journal ArticleDOI

Visible-Light-Catalyzed N-Radical-Enabled Cyclization of Alkenes for the Synthesis of Five-Membered N-Heterocycles.

TL;DR: In this paper, the authors classified intramolecular cyclization and intermolecular N-centered radical addition/cyclization reactions into five-membered N-heterocycles and showed the significant developments in this promising field, including the selection of catalysts, substrate scope, mechanistic understanding and applications.
References
More filters
Journal ArticleDOI

Fluorine in Pharmaceuticals: Looking Beyond Intuition.

TL;DR: Experimental progress in exploration of the specific influence of carbon-fluorine single bonds on docking interactions is reviewed and complementary analysis based on comprehensive searches in the Cambridge Structural Database and the Protein Data Bank is added.
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.
Journal ArticleDOI

Understanding organofluorine chemistry. An introduction to the C–F bond

TL;DR: Fundamental aspects of the C-F bond are explored to rationalise the geometry, conformation and reactivity of individual organofluorine compounds.
Related Papers (5)