Nickel-Catalyzed N-Arylation of Amides with (Hetero)aryl Electrophiles by Using a DBU/NaTFA Dual-Base System
作者:Mark Stradiotto、Travis Lundrigan、Joseph P. Tassone
DOI:10.1055/a-1337-6459
日期:2021.10
The first nickel-catalyzed N-arylation of amides with (hetero)aryl (pseudo)halides employing an organic amine base is described. When using Ni(COD)2/CyPAd-DalPhos catalyst mixtures in combination with DBU/NaTFA as a dual-base system, a diversity of (hetero)arylchloride, bromide, tosylate, and mesylate electrophiles were successfully cross-coupled with structurally varied primary amides, as well as
Use of compounds of formula (I) in the manufacture of a medicament for use in treating a disorder mediated by histone deacetylase: wherein the symbol ---- represents a single bond or a double bond or the symbol ---- R6 and R8 together represent cyclopropyl and R1 to R8 W, X and Y are as defined herein; and pharmaceutically acceptable salts thereof. Also disclosed are compounds for such uses. The compounds are useful in the treatment of cancers. They may be utilised in combination therapies with DNA methylation inhibitors and other anti cancer agents.