Physical Sciences and Mathematics Commons^™

Trichloroacetimidates As Outstanding Electrophiles For The Carbon-Nitrogen, Carbon-Oxygen And Carbon-Carbon Bonds Formation And Synthetic Studies Of Protein Phosphatase-5 (Pp5) Small Molecule Inhibitors, Nilamber Mate

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Trichloroacetimidates have been previously used for glycosidic bond formation in carbohydrate chemistry and in Friedel-Craft reactions. Traditionally, trichloroacetimidates had be synthesized using an alcohol and strongly basic conditions, but in recent years milder preparation methods have been reported. Given the ease of preparation of these versatile reagents, their chemistry has been explored intensely in recent years. While few reported methods suggest they can react under promoter free conditions, activation by Lewis or Brønsted acid leads to a formation of a carbocation from benzylic trichloroacetimidates. Work described herein makes use of these convenient carbocation precursors for new reactions.Isatin is an ambidentate …

Synthetic Studies On Small Molecule Modulators Of Src Homology 2 (Sh2) Domain-Containing Inositol 5’-Phosphatase (Ship), Otto Milhous Dungan

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Small molecule modulators of SH2-containing inositol 5’-phosphatase (SHIP) have recently become a hotly pursued area in medicinal chemistry. Pharmaceutical targeting of SHIP with small molecules has been identified as a new method to directly influence the phosphoinositide 3-kinase (PI3K) cell signaling pathway. Modulation of this pathway may be utilized in the development of interesting new therapeutics. A better understanding of the role that SHIP phosphatase activity plays in a number of disease states ranging from cancer to autoimmune disease to obesity may be ascertained by use of small molecule inhibitors. These investigations involved the synthesis of aminosteroid inhibitors and a …

Chimera Ligand For Pili And Lectin A Protein Controls Antibiotic-Promoted Biofilm Formation, Swarming Motility, Tolerance And Persister Formation By Pseudomonas Aeruginosa, Hewen Zheng

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Throughout the human history, the fight against bacterial infections had never stopped but the remedies for bacterial infections were often insufficient and for many infectious diseases, there was no treatment available. The revolution in antimicrobial infection therapy began with the discovery of penicillin by Alexander Fleming in 1928. However, since the first introduction of antibiotics, bacteria over time have evolved sophisticated resistant strains against almost all the available antibiotics which cause selection pressure on the bacteria to evolve their genetic makeup and develop resistance against such agents. Furthermore, bacteria can form surface attached multicellular communities known as biofilms. Bacteria residing …

Thioetherification And Etherification Utilizing Trichloroacetimidates Under Thermal Conditions & Progress Towards An Efficient Synthesis Of Aqx-1125, Brian C. Duffy

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The synthesis of ethers and thioethers is necessary as the motifs are ubiquitous in natural products, pharmaceuticals, and are quite useful in numerous synthetic applications. While common methodologies prepare simple ether and thioether substrates, the harsh conditions of these techniques make them unsuitable for complex molecules. The requirement for these functional groups to be prepared by facile and efficient means has led to an investigation into O - and S – alkylations occurring solely under thermal conditions utilizing trichloroacetimidates.

The alkylation of thiols by the direct displacement of trichloroacetimidates has been accomplished under thermal conditions (heating in refluxing THF). These …