ABSTRACT
A systematic investigation of the interaction of microwave irradiation with microcrystalline cellulose has been carried out, covering a broad temperature range (150 â 270 °C). A variety of analytical techniques (e.g., HPLC, (13)C NMR, FTIR, CHN analysis, hydrogen-deuterium exchange) allowed for the analysis of the obtained liquid and solid products. Based on these results a mechanism of cellulose interaction with microwaves is proposed. Thereby the degree of freedom of the cellulose enclosed CH2OH groups was found to be crucial. This mechanism allows for the explanation of the different experimental observations such as high efficiency of microwave treatment; the dependence of the selectivity/yield of glucose on the applied microwave density; the observed high glucose to HMF ratio; and the influence of the degree of cellulose crystallinity on the results of the hydrolysis process. The highest selectivity toward glucose was found to be ~75% while the highest glucose yield obtained was 21%.
Subject(s)
Cellulose/chemistry , Glucose/chemistry , Microwaves , PolymerizationABSTRACT
We have developed a heterogeneous silica catalyst that can effectively catalyse amide synthesis from acid and amine, without production of toxic by-products and with the advantage of being readily available, low cost, environmentally benign and reusable.
Subject(s)
Amides/chemical synthesis , Green Chemistry Technology/economics , Green Chemistry Technology/methods , Acetamides/chemical synthesis , Acetamides/chemistry , Amides/chemistry , CatalysisABSTRACT
In the search for opioid agonists with delayed antagonist actions as potential treatments for substance abuse, the bridged morphinan BU74 (17-cyclopropylmethyl-3-hydroxy-[5beta,7beta,3',5']-pyrrolidino-2'[S]-phenyl-7alpha-methyl-6,14-endoetheno morphinan) (3f) was synthesized. In isolated tissue and [35S]GTPgammaS opioid receptor functional assays BU74 was shown to be a potent long-lasting kappa opioid receptor agonist, delta opioid receptor partial agonist and mu opioid receptor antagonist. In antinociceptive tests in the mouse, BU74 showed high efficacy and potent kappa opioid receptor agonism. When its agonist action had waned BU74 became an antagonist of kappa and mu opioid receptor agonists in the tail flick assay and of delta, kappa and mu opioid receptor agonists in the acetic acid writhing assay. The slow onset, long-duration kappa opioid receptor agonist effects of BU74 suggests that it could be a lead compound for the discovery of a treatment for cocaine abuse.
Subject(s)
Bridged-Ring Compounds/pharmacology , Morphinans/pharmacology , Receptors, Opioid, kappa/agonists , Acetic Acid , Analgesics/pharmacology , Animals , Benzomorphans/pharmacology , Binding, Competitive/drug effects , Bridged-Ring Compounds/chemistry , Cell Line, Tumor , Guanosine 5'-O-(3-Thiotriphosphate)/metabolism , Guinea Pigs , Hot Temperature/adverse effects , Ileum/drug effects , Ileum/metabolism , In Vitro Techniques , Male , Mice , Mice, Inbred ICR , Morphinans/chemistry , Narcotic Antagonists/pharmacology , Pain/chemically induced , Pain/etiology , Pain/prevention & control , Pain Measurement , Radioligand Assay , Receptors, Opioid, delta/agonists , Receptors, Opioid, delta/antagonists & inhibitors , Receptors, Opioid, delta/metabolism , Receptors, Opioid, kappa/antagonists & inhibitors , Receptors, Opioid, kappa/metabolism , Receptors, Opioid, mu/agonists , Receptors, Opioid, mu/antagonists & inhibitors , Receptors, Opioid, mu/metabolism , Sulfur Radioisotopes , Vas Deferens/drug effects , Vas Deferens/metabolismABSTRACT
The development of buprenorphine as a treatment for opiate abuse and dependence has drawn attention to opioid ligands that have agonist actions followed by long-lasting antagonist actions. In a search for alternatives to buprenorphine, we discovered a bridged pyrrolidinomorphinan (BU72). In vitro, BU72 displayed high affinity and efficacy for mu-opioid receptors, but was also a partial delta-opioid receptor agonist and a full kappa-opioid receptor agonist. BU72 was a highly potent and long-lasting antinociceptive agent against both thermal and chemical nociception in the mouse and against thermal nociception in the monkey. These effects were prevented by mu-, but not kappa- or delta-, opioid receptor antagonists. Once the agonist effects of BU72 had subsided, the compound acted to attenuate the antinociceptive action of morphine. BU72 is too efficacious for human use but manipulation to reduce efficacy could provide a lead to the development of a treatment for opioid dependence.
Subject(s)
Morphinans/pharmacology , Pyrroles/pharmacology , Receptors, Opioid, mu/antagonists & inhibitors , Analgesics/pharmacology , Animals , Binding, Competitive/drug effects , Buprenorphine/metabolism , Buprenorphine/pharmacology , CHO Cells , Cell Line, Tumor , Cricetinae , Cricetulus , Dose-Response Relationship, Drug , Female , Guanosine 5'-O-(3-Thiotriphosphate)/metabolism , Guinea Pigs , Ileum/drug effects , Ileum/physiology , In Vitro Techniques , Macaca mulatta , Male , Mice , Mice, Inbred ICR , Morphinans/chemistry , Morphinans/metabolism , Morphine/metabolism , Morphine/pharmacology , Muscle Contraction/drug effects , Pain/prevention & control , Pain Measurement/methods , Pyrroles/metabolism , Radioligand Assay , Rats , Receptors, Opioid, delta/metabolism , Receptors, Opioid, kappa/metabolism , Receptors, Opioid, mu/metabolism , Sulfur Radioisotopes , Time Factors , Tritium , Vas Deferens/drug effects , Vas Deferens/physiologyABSTRACT
The low temperature microwave activation of biomass has been investigated as a novel, energy efficient route to bio-oils. The properties of the bio-oil produced were considered in terms of fuel suitability. Water content, elemental composition and calorific value have all been found to be comparable to and in many cases better than conventional pyrolysis oils. Compositional analysis shows further differences with conventional pyrolysis oils including simpler chemical mixtures, which have potential as fuel and chemical intermediates. The use of simple additives, e.g. HCl, H(2)SO(4) and NH(3), affects the process product distribution, along with changes in the chemical composition of the oils. Clearly the use of our low temperature technology gives significant advantages in terms of preparing a product that is much closer to that which is required for transport fuel applications.