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-9422232-B2 优先权日:2009-07-09 标题:Reductive release probes containing a chemoselectively cleavable α-azidoether linker and methods of use thereof 发明人:FRANZINI RAPHAEL M; KOOL ERIC TODD 权利人:FRANZINI RAPHAEL M; KOOL ERIC TODD; UNIV LELAND STANFORD JUNIOR 摘要:Probes comprising one or more selectively cleavable α-azidoether moieties are provided; and linkers comprising the one or more selectively cleavable α-azidoether moieties. The α-azidoether moiety will undergo a Staudinger reaction with a suitable reducing agent, resulting in cleavage. The probes find use in a variety of detection assays, e.g. specific polynucleotide binding assays, polypeptide binding assays, etc. The cleavable linkers are suitable for synthetic reactions, e.g. to prepare probes of the invention; in the synthesis of cleavable peptide conjugates; and the like.
专利号:EP-1575990-B1 优先权日:2002-09-08 标题:Solid phase bound PNA-dimers and their synthesis 发明人:CASALE RALPH A; COULL JAMES M; DEY SUBHAKAR; KOWALCZYK BRUCE A; GAN KEVIN Z 权利人:APPLERA CORP 摘要:This invention pertains to the field of PNA dimer and PNA oligomer synthesis.
专利号:EP-1575990-A4 优先权日:2002-09-08 标 题:METHODS, COMPOSITIONS AND BANKS RELATING TO THE SYNTHESIS OF DIMER AND OLIGOMER OF ANP
专利号:WO-2013112215-A1 优先权日:2012-01-24 标题:Synthesis, dye functionalization and bioimaging of polymeric nanocapsules 发明人:BALASUBRAMANIAN RAMJEE; OSGOOD CHRISTOPHER; MAHADEVAN KALPANA; PATTHIPATI VANKATA SURESH; HAN SANGBUM; SWANSON JAMES 权利人:OLD DOMINION RES FOUNDATION; BALASUBRAMANIAN RAMJEE; OSGOOD CHRISTOPHER; MAHADEVAN KALPANA; PATTHIPATI VANKATA SURESH; HAN SANGBUM; SWANSON JAMES 摘要:The present invention relates to functionalized polymeric nanocapsules, methods of making thereof and use thereof in. bio-imaging systems. I n particular, the functionalized nanocapsules of the invention may be formed by thiol -en e photopolymerization of resorcinarene derviatives, wherein the resulting nanocapsule products are further functionalized. with moieities having properties, such as, water solubility and/or fluorescence.
专利号:WO-9740030-A1 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
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合成参考文献
参考文献:10.1186/1746-6148-7-39 摘要:Jana K, Samanta PK. Clinical Evaluation of Non-surgical Sterilization of Male Cats with Single Intra-testicular Injection of Calcium Chloride. BMC Veterinary Research. 2011 Jul 21;7(1):39. doi: 10.1186/1746-6148-7-39.