Palladium‐Catalyzed Regioselective Coupling of Amidines and 1,2,3‐Triiodobenzenes: Facile Synthesis of 2,3‐Diiodinated N‐Arylbenzimidamides as Potential MDM2 and MDM4 Inhibitors
Abstract:A facile and unprecedented synthesis of 2,3-diiodinated Narylbenzimidamide derivatives through highly regioselective Buchwald-Hartwig coupling of 5-substituted-1,2,3-triiodobenzene and amidine is described. Remarkably, the amination reactions are proceeded exclusively at the terminal positions, the less sterically hindered, and the most regioactive positions. The highest yields were isolated from a combination between electron-poor 1,2,3-triiodoarenes and electron-poor benzimidamides. The optimized conditions … Show more
“…Compound 117 was introduced as the most effective derivative as a potential compound for MDM2 and MDM4 activity-related disease therapy. 194 Its large-scale synthesis comprises two main steps C–N bond formation and ring-closing metathesis reaction.…”
Section: C–n Cross-coupling Reactions In Pharmaceutical Compoundsmentioning
C–N cross-coupling bond formation reactions have become valuable approaches to synthesizing anilines and their derivatives which are known as important chemical compounds.
“…Compound 117 was introduced as the most effective derivative as a potential compound for MDM2 and MDM4 activity-related disease therapy. 194 Its large-scale synthesis comprises two main steps C–N bond formation and ring-closing metathesis reaction.…”
Section: C–n Cross-coupling Reactions In Pharmaceutical Compoundsmentioning
C–N cross-coupling bond formation reactions have become valuable approaches to synthesizing anilines and their derivatives which are known as important chemical compounds.
A simple and direct synthesis of 2,6-diiodophenylethanol building blocks through highly regioselective metalation (MIE)/oxirane SN2-type ring opening of 1,2,3-triiodobenzene is described. A significant impact of the nature of the R1...
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