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Mild methods for conducting Knorr chemistry with beta-ketonitriles were developed. This enabled the preparation of 4-cyanopenta-substituted pyrroles and gave access to alpha-amino-3-hydroxy- 5-methyl-4-isoxazolepropionic acid ( AMPA) receptor potentiators for biological evaluation. In addition, a series of alkyl and aryl beta-ketonitriles were employed in Knorr cyclizations to probe steric tolerance and the possibility of direct introduction of aromatic moieties via Knorr chemistry.

PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate template. Several compounds in this series have demonstrated potent plasma glucose and triglyceride lowering capability in rodent models of type 2 diabetes.

Echinocandin B (ECB) analog 1c was methylphosphonylated with the new reagent dimethyldiphosphonate 7. Selective functionalization of the phenol group was achieved in the presence of 11 other reactive alcohol and amide groups. The phosphonylation was best conducted in a mixture of THF and DMF using lithium t-butoxide as base. Methylphosphonate diester 1d was deprotected by hydrogenolysis to afford methylphosphonate monoester 1e, a potential prodrug for ECB analog 1c.