Tuesday, March 17, 2015

John Weigel on Click Chemistry and Microwaves or Ultrasound Irradiation

Ladies and Gentlemen,

 Is this a "smoking gun" regarding the effects of microwave radiation and infrasound resulting in vibroacoustic disease?

 The argument that artificial electromagnetic radiation does not affect human beings - and Nature in general - is undermined by evidence from another discipline: chemistry. 

 The concept of “Click Chemistry” was first coined K. B. Sharpless in 1998. It was first fully described by Sharpless, Hartmuth Kolb, and M.G. Finn of The Scripps Research Institute in 2001.

Click Chemistry Under Microwave or Ultrasound Irradiation

 This process is currently in use by Big Pharma to create pharmaceuticals in which interaction with microwaves and ultrasound are substitutes for heat to combine molecules.

 Click Chemistry, in which which molecules "click" together following microwave exposure, raises three issues:
  1. what effects are being created outside the controlled conditions of a pharmaceutical lab;  
  2. the issue of heat renders SAR values questionable as argued by Dr. Dimitris Panagopoulos, Prof. Olle Johansson and Dr. George Carlo last year; and
  3. how, at a molecular level, does the use of ultrasound - the military's ground wave technology (GWEN) - relate to acoustic issues associated wind turbines?
 Logically, if science can harness the interaction of microwave radiation / sound waves and molecules, these frequencies should have an effect outside the laboratory on the entire planet.

 Thank you to Alex Campbell of the Dublin Institute of Technology, Kevin Street, Dublin, Ireland for noting the Click Chemistry process.

John Weigel  

Click Chemistry Under Microwave or Ultrasound Irradiation  
Author(s): Alessandro Barge, Silvia Tagliapietra, Arianna Binello and Giancarlo Cravotto  
Pages 189-203 (15) 
The copper-catalyzed azide-alkyne cycloaddition (CuAAC) is generally recognized as the most striking example of “click reaction”. CuAAC fit so well into Sharpless definition that it became almost synonymous with “click chemistry” itself. The most common catalyst systems employ Cu(II) salt in the presence of a reducing agent (i.e. sodium ascorbate) to generate the required Cu(I) catalyst in situ or as an alternative the comproportionation of Cu(II)/Cu(0) species. Although, Cu(I) catalyzes the reaction with a rate enhancement of 107 even in the absence of ligands and provides a clean and selective conversion to the 1,4-substituted triazoles, some bulky and scantily reactive substrates still require long reaction times and often few side products are formed. Outstanding results have been achieved by performing CuAAC under microwave (MW) irradiation. Several authors described excellent yields, high purity and short reaction times. In few cases also power ultrasound (US) accelerated the reaction, especially when heterogeneous catalysts or metallic copper are employed. The aim of this review is to summarize and highlight the huge advantages offered by MW- and US-promoted CuAAC. In the growing scenario of innovative synthetic strategies, we intend to emphasize the complementary role played by these non-conventional energy sources and click chemistry to achieve process intensification in organic synthesis. 

Click chemistry, microwave, ultrasound, organic synthesis, green chemistry, Ultrasound Irradiation, copper-catalyzed azide-alkyne cycloaddition, click re-action, 1,4-substituted triazoles, microwave (MW) irradiation, 1,3-dipolar Huisgen cycloaddition, macro-cyclic structures, oxidation, reduction, hydrolysis, peptidomimet-ics, bioconjugation, combinato-rial drug discovery, nucleosides, oligonucleotides, bioisosteres, active moieties, bioorthogonal reac-tions, carbohydrate-based drug discovery, glycobiology, rotaxanes, catenane, sonochemical conditions, Peptides, Liskamp's group, bis-propinoxybenzoic acid, azidoacid, azidopep-tide, cyclic-RGD (Arg-Gly-Asp tripeptide), non-hydrolysable isoster, Fmoc-protected small peptidomimetics, 1,3 dipolar cycloaddition, acetylenic amide, silica-gel chromatography, N-Boc-amino-alkyne, Boc cleavage, tissue engineering, novel bio-materials, dipeptide azido-phenylalanyl-alanyl-propargyl, mer-capto, hydroxy, carboxylic groups, nucleic acid, triplex-forming, oligonucleotides (TFOs), peptide nucleic, DNA, Saccharide Conjugation, Oligo- and Polysaccharides, Glycosilated aminoacids, linear oligomer, cyclic dimer, ethynylpyrazinone, azido saccharide, azido-functionalized, phosphoramidate bonds, DNA based glycoclusters, Propargylated pentaerythrityl phosphodiester oligomers, bis-propargylated pentaerythritol-based phosphoramidite, ascorbic, Glycodendrimers, heptavalent glycocy-clodexrins, propargyl, thiopropargyl mannose, ascorbic acid catalytic system, Heptakis-azido-cyclodextrin, gold nanoparticles, poli-azido gold, 1'azido-2',3',5',tri-O-acetylribose, ruthenium-catalyzed, Ru-catalyzed click reactions, Bronsted acid, 2-azido-4,4-bis-hydroxymethylcyclopentanole, carbanucleosides, tetrakis(acetonitrile)copper hexafluorophos-phate ([Cu(CH3CN)4]PF6), imidazoline(mesythyl) copper bro-mide (Imes)CuBr, enzymatic depolymerization, thymidine dimer, in situ, Miscellaneous, [1,5-a]azocine skeleton, a potent antileukemic, tubu-lin polymerization, stereochemistry, diastereoisomer, organic azides, Biginelli's multicomponent reaction, triazolyl-quinolones 

Dipartimento di Scienza e Tecnologia del Farmaco, Universita di Torino, Via Giuria 9 -10125- Torino, Italy.

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