Late‐Stage Amination of Drug‐Like Benzoic Acids: Access to Anilines and Drug Conjugates through Directed Iridium‐Catalyzed C−H Activation

Autor:	Magnus Johansson, Belén Martín-Matute, Erik Weis
Rok vydání:	2021
Předmět:	Drug Aniline Compounds Chemistry Drug discovery media_common.quotation_subject Organic Chemistry Chemical biology General Chemistry Iridium Benzoates Combinatorial chemistry Catalysis Pharmaceutical Preparations Targeted drug delivery Molecule Amination media_common Conjugate
Zdroj:	Chemistry – A European Journal. 27:18188-18200
ISSN:	1521-3765 0947-6539
Popis:	Functionalization of C-H bonds, ubiquitous in drugs and drug-like molecules, represents an important synthetic strategy with a potential to streamline the drug discovery process. Late-stage aromatic C-N bond forming reactions are highly desirable, but despite their significance, accessing aminated analogues through direct and selective amination of C-H bonds remains a challenging goal. The herein presented method enables the amination of a wide array of benzoic acids with high selectivity. The robustness of the system is manifested by the large number of functional groups tolerated, which allowed for the amination of a diverse array of marketed drugs and drug-like molecules. Furthermore, the introduction of a synthetic handle enabled expeditious access to targeted drug delivery conjugates, PROTACs, as well as probes for chemical biology. The rapid access to valuable analogues, combined with operational simplicity and applicability to high-throughput experimentation has the potential to aid, and considerably accelerate, drug discovery.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::742fded8ff4b6f22bb4dfeb08c9b5bdb https://doi.org/10.1002/chem.202103510 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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