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2-(Trifluoromethyl)indoles via Pd(0)-Catalyzed C(sp(3))-H Functionalization of Trifluoroacetimidoyl Chlorides

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Nicolai Cramer, Julia Pedroni
2016
journal articles

Abstract

Perfluoroalkylated indoles are valuable compounds in drug discovery. A Pd(0)-catalyzed C(sp(3))-H functionalization enables access to 2-(trifluoromethyl)indoles from trifluoroacetimidoyl chlorides. These are stable compounds, easily obtained from anilines. The cyclization operates with catalyst loadings as low as 1 mol % and accommodates a variety of substituents.

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https://infoscience.epfl.ch/entities/publication/7c87cadb-1e0f-4431-936b-203a021e45d3

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Related concepts (21)

In the fields of medicine, biotechnology and pharmacology, drug discovery is the process by which new candidate medications are discovered. Historically, drugs were discovered by identifying the active ingredient from traditional remedies or by serendipitous discovery, as with penicillin. More recently, chemical libraries of synthetic small molecules, natural products or extracts were screened in intact cells or whole organisms to identify substances that had a desirable therapeutic effect in a process known as classical pharmacology.

Abelian variety

In mathematics, particularly in algebraic geometry, complex analysis and algebraic number theory, an abelian variety is a projective algebraic variety that is also an algebraic group, i.e., has a group law that can be defined by regular functions. Abelian varieties are at the same time among the most studied objects in algebraic geometry and indispensable tools for much research on other topics in algebraic geometry and number theory. An abelian variety can be defined by equations having coefficients in any field; the variety is then said to be defined over that field.

Algebraic variety

Algebraic varieties are the central objects of study in algebraic geometry, a sub-field of mathematics. Classically, an algebraic variety is defined as the set of solutions of a system of polynomial equations over the real or complex numbers. Modern definitions generalize this concept in several different ways, while attempting to preserve the geometric intuition behind the original definition. Conventions regarding the definition of an algebraic variety differ slightly.

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