Leibnizinstitut Für Naturstoff-Forschung Und Infektionsbiologie E. V. -Hans-Knöll-Institut

Veit Haensch

Christian Hertweck

Florian Kloss

Toni Neuwirth

The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar&#x2014;Ar' by photochemically reacting a precursor compound of formula (II): Ar&#x2014;L&#x2014;Ar&#x2032; to form a biaryl compound of general formula: Ar&#x2014;L&#x2014;Ar&#x2032;(II)&#x2192;Ar&#x2014;Ar&#x2032; (I) wherein Ar and Ar&#x2032;, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group &#x2014;X&#x2014;Y&#x2014;Z&#x2014; as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.

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Jena, Germany

Veit Haensch