专利号:US-8314015-B2 优先权日:2010-07-14 标题 :Silicon surface modification for the electrochemical synthesis of silicon particles in suspension 发明人:TU CHANG-CHING; TANG LIANG; VOUTSAS APOSTOLOS T 权利人:TU CHANG-CHING; TANG LIANG; VOUTSAS APOSTOLOS T; SHARP LAB OF AMERICA INC 摘要:A process of silicon (Si) surface modification is provided for the electrochemical synthesis of Si particles in suspension. The process begins with a Si first substrate with a surface, and forms Si particles attached to the surface. Hydrogen-terminated Si particles are created and the first substrate is immersed in a hexane/1-octene (1/1 volume ratio) solution with a catalytic amount of chloroplatinic acid (H 2 PtCl 6 ). 1-octene is bonded with the hydrogen-terminated Si particles, creating modified Si particles, with octane capping ligands, attached to the substrate surface. The first substrate is then exposed to ultrasonication, separating the modified Si particles from the first substrate. After removing the first substrate, a suspension is created of modified Si particles suspended in excess hexane/1-octene.
专利号:WO-9837078-A1 优先权日:1997-02-20 标题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The thiophenes are prepared by reaction of a substrate-bound primary or secondary amine with a thiophosgene equivalent and reaction of the resulting intermediate with an acceptor-substituted acetonitrile in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegler-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:WO-9740025-A1 优先权日:1996-04-19 标 题 :Solid phase and combinatorial synthesis of substituted 1,2,3-triazoles and of arrays of substituted 1,2,3-triazoles 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS; DOERWALD FLORENCIO ZARAGOZA 摘要:A solid phase method for the synthesis of a plurality of differently substituted 1,2,3-triazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 1,2,3-triazoles are prepared by acylation of a substrate-bound primary or secondary amine with a 3-oxoalkanoic acid and reaction of the resulting amide with a primary amine under dehydrating conditions to give an enamine. Treatment of this substrate-bound enamine with a sulfonyl azide in the presence of a base gives the corresponding 1,2,3-triazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 1,2,3-triazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse triazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-6136984-A 优先权日:1996-04-22 标 题 :Solid phase and combinatorial synthesis of substituted thiophenes and of arrays of substituted thiophenes 发明人:DOERWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted thiophenes with a wide variety of side-chain substituents as compounds of potential therapeutic interest is disclosed. The thiophenes are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide, followed by Thorpe-Ziegier-cyclization yields differently substituted, support-bound 3-aminothiophenes. These may be screened on the substrate or cleaved from the substrate and then screened in solution. Alternatively, the resin-bound 3-amino thiophenes or the synthetic intermediates can be subjected to further synthetic transformations (N-acylation, reduction) on the support, which permits the preparation of further therapeutically interesting compounds. The efficient synthesis of a wide variety of thiophenes using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiophene-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-5847150-A 优先权日:1996-04-24 标题 :Solid phase and combinatorial synthesis of substituted 2-methylene-2, 3-dihydrothiazoles and of arrays of substituted 2-methylene-2, 3-dihydrothiazoles 发明人:DORWALD FLORENCIO ZARAGOZA 权利人:NOVO NORDISK AS 摘要:A solid phase method for the synthesis of a plurality of differently substituted 2-methylenethiazoles with a wide variety of side-chain substituents as compounds of potential therapeutic interest. The 2-methylenethiazoles are prepared by acylation of a substrate-bound primary or secondary amine with cyanoacetic acid and reaction of the resulting cyanoacetamide with an isothiocyanate in the presence of a base. Alkylation with an appropriate alkyl halide under acidic conditions yields differently substituted, support-bound 2-methylene-2,3-dihydrothiazoles. These may be screened on the substrate or cleaved from the substrate and then screened in solution. The efficient synthesis of a wide variety of 2-methylenethiazoles using automated synthesis technology of the present method makes these compounds attractive candidates for the generation and rapid screening of diverse thiazole-based libraries. The method disclosed here provides an easy and fast access to highly diverse heterocyclic compounds of therapeutic interest, amenable to automatization.
专利号:US-2005019901-A1 优先权日:2002-01-31 标题 :Methods for synthesis of bio-active nanoparticles and nanocapsules for use in optical bio-disc assays and disc assembly including same 发明人:MATVEEVA EVGENIA; VALENCIA RAMONCITO MAGPANTAY; WERNER MARTINA ELISABETH 摘要:Optical bio-disc assays and synthesis of bio-active nanoparticles and nanocapsules for use therewith. Related methods for synthesis of polymeric nanoparticles for use in disc assays include forming reverse micelles having an outer non-polar shell and an inner polar cavity and solubilizing in the reverse micelles a polymerizing mixture including monomers, co-monomers, weakly polar monomers, and/or polymerizable surfactants. This may also include an initiator of polymerization. The methods also include polymerizing the mixture. The invention is also directed to the use of the nanoparticles and nanocapsules in optical bio-disc assays for the detection of analytes including nucleic acid sequences. Related optical assay discs and disc systems are also provided.
[参考文献]: Yukitaka Nakano, Et Al. Liquid Chromatographic Determination Of Ethambutol In Serum Samples Based On Intramolecular Excimer-Forming Fluorescence Derivatization. Anal Sci. 2004 Mar;20(3):489-93.
合成参考文献
摘要:Shimada, K., Science of Synthesis Knowledge Updates, (2013) 2, 303. 摘要:R. Näsänen and P. Merilainen. Suomen Kemistilehti B 36, 205 (1963).