34161-81-4Relevant articles and documents
Late-Stage Amination of Drug-Like Benzoic Acids: Access to Anilines and Drug Conjugates through Directed Iridium-Catalyzed C?H Activation
Weis, Erik,Johansson, Magnus J.,Martín-Matute, Belén
supporting information, p. 18188 - 18200 (2021/11/22)
The functionalization of C?H bonds, ubiquitous in drugs and drug-like molecules, represents an important synthetic strategy with the 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 method presented herein 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 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, and probes for chemical biology. This 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.
Method for Preparing Derivatives of Anthranilic acid and Anti-inflammatory Use Thereof
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Paragraph 0058; 0065-0073; 0124, (2018/11/27)
The present invention relates to a production method of anthranilic acid derivatives which reacts benzoic acid derivatives and phenylsulfonyl azide derivatives under the presence of a [IrCp*Cl_2]_2 catalyst; and relates to an anti-inflammatory use of the
Metal-free synthesis of 1H-indole-2-carbaldehydes by N-iodosuccinimide- mediated cyclization of 1-(2′-anilinyl)prop-2-yn-1-ols in water. A formal synthesis of (R)-calindol
Kothandaraman, Prasath,Lauw, Sherman Jun Liang,Chan, Philip Wai Hong
, p. 7471 - 7480 (2013/08/23)
A N-iodosuccinimide (NIS)-mediated method to prepare 1H-indole-2- carbaldehydes efficiently from cycloisomerization of 1-(2-aminophenyl)prop-2-yn- 1-ols is described. The reaction is operationally straightforward and accomplished in good to excellent yiel