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Relevant academic research and scientific papers

Tungsten-Catalyzed Transamidation of Tertiary Alkyl Amides

Transamidation has recently emerged as a straightforward and convenient means to diversify amides. However, the kinetically and thermodynamically demanding transamidation of notoriously robust, fully alkyl-substituted tertiary amides still remains a longstanding challenge. Here, we describe a method for the activation of tertiary alkyl amides to streamline transamidation using simple tungsten(VI) chloride as a catalyst and chlorotrimethylsilane as an additive. The highly electrophilic and oxophilic tungsten catalyst enables the selective scission of a C-N bond of tertiary alkyl amides to effect transamidation of a myriad of structurally and electronically diverse tertiary alkyl amides and amines. Mechanistic study implies that the synergistic effect of the catalyst and the additive could pronouncedly induce the nucleophilic acyl substitution of tertiary alkyl amide with amine to realize transamidation.

NOVEL INHIBITORS OF HISTONE DEACETYLASE FOR THE TREATMENT OF DISEASE

Disclosed herein are carbonyl compounds of Formula: (I) as described herein. Compounds as modulators of histone deacetylase (HDAC), pharmaceutical compositions comprising the same, and methods of treating disease using the same are disclosed.