- SUBSTITUTED 6,7-DIALKOXY-3-ISOQUINOLINOL DERIVATIVES AS INHIBITORS OF PHOSPHODIESTERASE 10 (PDE10A)
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The invention relates to compounds of the formula wherein R′, R1, through R7 and Ar are as defined herein. These compounds are useful as inhibitors of phosphodiesterase 10 (PDE10A) which are useful in treating central nervous system diseases such as psychosis and also in treating, for example, obesity, type II diabetes, metabolic syndrome, glucose intolerance, pain and ophthalmic diseases.
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Page/Page column 83
(2012/09/05)
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- Water-soluble group III polyether acid salt complexes and thin films from same
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A water-stable and water-soluble ceramic precursor is provided, containing at least one Group III element. Also, a metal acid salt complex is provided comprising (1) bismuth, lanthanum, and titanium, and (2) a polyether acid. In addition, methods are provided for preparing the Group III metal acid salt complex and the Bi, La, Ti acid salt complex comprising a bismuth polyether acid salt complex, a lanthanum polyether acid salt complex, and a titanium polyether acid salt complex. Finally, devices that include lanthanum-doped bismuth titanate as the active component are provided, as well as a water-stable and water-soluble gallium polyether acid complex.
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Page/Page column 6
(2008/06/13)
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- Synthesis and biological investigation of new 4″-malonyl tethered derivatives of erythromycin and clarithromycin
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A new approach to 4″-substituted derivatives of erythromycin and clarithromycin was developed by converting them into corresponding 4″-malonic monoesters. Subsequent carbodiimide coupling with alcohols and amines provided new macrolide derivatives that are capable of binding to 50S ribosomal subunits and inhibiting protein synthesis in cell-free system.
- Sherman, Daniel,Xiong, Liqun,Mankin, Alexander S.,Melman, Artem
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p. 1506 - 1509
(2007/10/03)
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- An Effective Use of Benzoic Anhydride and Its Derivatives for the Synthesis of Carboxylic Esters and Lactones: A Powerful and Convenient Mixed Anhydride Method Promoted by Basic Catalysts
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Various carboxylic esters are obtained at room temperature in excellent yields with high chemoselectivities from nearly equimolar amounts of carboxylic acids and alcohols using 2-methyl-6-nitrobenzoic anhydride with triethylamine by the promotion of a basic catalyst such as 4-(dimethylamino)pyridine. A variety of lactones are also prepared in high yields at room temperature from the corresponding ω-hydroxycarboxylic acids with use of 2-methyl-6-nitrobenzoic anhydride in the presence of 4-(dimethylamino)pyridine. A similar reaction occurs with triethylamine when using a catalytic amount of 4-(dimethylamino)pyridine 1-oxide as an effective promoter for the intramolecular condensation reaction. These methods are successfully applied to the synthesis of erythro-aleuritic acid lactone and an eight-membered-ring lactone moiety of octalactins A and B. The efficiency of the cyclizations is compared to those of other reported lactonizations.
- Shiina, Isamu,Kubota, Mari,Oshiumi, Hiromi,Hashizume, Minako
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p. 1822 - 1830
(2007/10/03)
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- Hydrogenation of 2-fluoro-9-(2,3,5-tri-o-benzyl-beta-D-arabinofuranosyl)adenine
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A process for the preparation of 2-fluoro-9-beta-D-arabinofuranosyl purine (VII) by a reaction of palladium chloride and hydrochloric acid with 2-fluoro-9-(2,3,5-tribenzyl-beta-D-arabinofuranosyl)adenine (VI) at elevated pressures in a solvent for (VI) is described. The reaction is rapid, economical and efficient.
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- Process for the preparation of 2-amino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl) adenine and novel intermediates
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A process for the preparation of 2,6-diamino-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)purine (V) by reacting 2,6-di(alkoxyacetamido)purine (II) with 2,3,5-tri-O-benzyl-1-chloro-alpha-D-arabinofuranose (III) to produce 2,6-di(alkoxyacetamido)-9-(2,3,5-tri-O-benzyl-beta-D-arabinofuranosyl)purine (IV) and then deprotecting the 2,6-positions to produce the 2,6-diamine (V) is described. The process provides purine (V) in high yield. Purine (V) is an intermediate in the preparation of 9-beta-D-arabinofuranosyl-2-fluoroadenine which is a cytotoxic agent.
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- Reversible reactions in the acidolysis of methoxyacetic acid by acetic anhydride
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Reversible reactions in the acidolysis of methoxyacetic acid by acetic anhydride were investigated by 1H NMR spectroscopy.The equilibrium constants were calculated and the absence of a temperature effect on their values was demonstrated.
- Utkin, A. Yu.,Bogel'fer, L. Ya.,Chimishkyan, A. L.
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p. 1049 - 1050
(2007/10/02)
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