专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-11407993-B2 优先权日:2017-02-14 标 题 :Method for the synthesis of DNA conjugates by micellar catalysis 发明人:BHAT AVINASH SHASHIDHAR; KLIKA SKOPIC MATEJA; BRUNSCHWEIGER ANDREAS; WEBERSKIRCH RALF 权利人:UNIV DORTMUND TECH 摘要:A method for the synthesis of a chimeric conjugate molecule by micellar catalysis that may form part of DNA-encoded compound libraries. A DNA-coupled organic starter molecule may be reacted with another organic compound, using a catalyst located within a micelle, to form a conjugate of an organic candidate compound coupled to a DNA identifier tag.
专利号:US-2013165350-A1 优先权日:2011-12-22 标 题:Surface linkers for array synthesis 发明人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR 权利人:KUIMELIS ROBERT; MCGALL GLENN; PAO DEXTER; CHEN ZIHUI; AXELROD TREVOR; AFFYMETRIX INC 摘要:The present invention provide several methods of derivatizing a surface of a support with one or more linkers thus providing a suitable platform for synthesis of a polymer array, particular a nucleic acid array. Some methods derivatize a surface with a self-assembled monolayer (SAM) of a linker. The SAM confers advantages of hydrolytic stability, broad compatibility with synthesis and detection chemistries, and reduced emergence of latent functional groups during polymer array synthesis. Substrates can also be derivatized with multi-layers of SAMs providing greater hydrolytic stability. Substrates can also be derivatized by synthesizing a linker in situ on the substrate by atom transfer radical polymerization of functional and functional monomers. Appropriate selection of monomers reduces emergence of latent functional groups in subsequent array synthesis.
专利号:US-9328109-B2 优先权日:2013-01-14 标 题:Process for the preparation of benzohetero [1, 3] diazole compounds disubstituted with heteroaryl groups 发明人:BIANCHI GABRIELE; PO' RICCARDO 权利人:ENI SPA 摘要:Process for the preparation of a benzohetero-[1,3]diazole compound disubstituted with brominated heteroaryl groups which comprises reacting at least one dihalogenated benzohetero[1,3]diazole compound with at least one brominated heteroaryl compound. Said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of compounds useful in the construction of solar concentrators (LSCs—“Luminescent Solar Concentratorsâ€?). Furthermore, said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used in the synthesis of photoactive polymers useful in the construction of photovoltaic devices (or solar devices) such as, for example, photovoltaic cells (or solar cells), photovoltaic modules (or solar modules), on both rigid or flexible supports. Furthermore, said benzohetero[1,3]diazole compound disubstituted with brominated heteroaryl groups can be advantageously used as precursor of monomeric units in the synthesis of semiconductr polymers.
专利号:US-2018361327-A1 优先权日:2016-02-26 标题 :Gas separation membrane, gas separation module, gas separator, gas separation method, composition for forming gas separation layer, method of producing gas separation membrane, polyimide compound, and diamine monomer 发明人:KODAMA KEISUKE; SAWADA MAKOTO; WADA KENJI 权利人:FUJIFILM CORP 摘要:A gas separation membrane including a gas separation layer contains a crosslinked polyimide compound. In the gas separation membrane, and a gas separation module, a gas separator, and a gas separation method obtained by using the gas separation membrane, the crosslinked polyimide compound has a specific structural portion. A composition for forming a gas separation layer suitable for forming a gas separation layer of the gas separation membrane; a method of producing a gas separation membrane obtained by using this composition; a polyimide compound suitable as a raw material of a gas separation layer of the gas separation membrane; and a diamine monomer suitable for synthesis of this polyimide compound are provided.
1: Brown A, Patel S, Ward C, Lorenz A, Ortiz M, DuRoss A, Wieghardt F, Esch A, Otten EG, Heiser LM, Korolchuk VI, Sun C, Sarkar S, Sahay G. PEG-lipid micelles enable cholesterol efflux in Niemann-Pick Type C1 disease-based lysosomal storage disorder. Sci Rep. 2016 Aug 30;6:31750. doi: 10.1038/srep31750. 2: Saifer MG, Williams LD, Sobczyk MA, Michaels SJ, Sherman MR. Selectivity of binding of PEGs and PEG-like oligomers to anti-PEG antibodies induced by methoxyPEG-proteins. Mol Immunol. 2014 Feb;57(2):236-46. doi: 10.1016/j.molimm.2013.07.014. Epub 2013 Nov 5. doi: 10.1517/17425247.2012.720969. Epub 2012 Aug 30.
合成参考文献
摘要:Ameduri, B., Science of Synthesis Knowledge Updates, (2014) 3, 332. 摘要:Verschueren, K. Handbook of Environmental Data on Organic Chemicals. Volumes 1-2. 4th ed. John Wiley & Sons. New York, NY. 2001, p. 2111 摘要:Lewis, R.J. Sr.; Hawley's Condensed Chemical Dictionary 14th Edition. John Wiley & Sons, Inc. New York, NY 2001., p. 721 摘要:ChemID 摘要:Lyman WJ et al; Handbook of Chemical Property Estimation Methods. Washington, DC: Amer Chem Soc pp. 7-4, 7-5, 8-12 (1990)