专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-2009171097-A1 优先权日:2005-11-22 标题 :Automated solid phase synthesis of pyrrole-imidazole polyamide 发明人:SUGIYAMA HIROSHI; DOHNO CHIKARA; FUKUDA NOBORU 权利人:SUGIYAMA HIROSHI; DOHNO CHIKARA; FUKUDA NOBORU 摘要:A synthesis method for pyrrole-imidazole polyamide is automated at a higher level and can produce a product with a high yield in a more stable manner. In a solid phase synthesis method, the automated synthesis of a polyimide can be promoted by using HCTU as a condensation-activator, the yield of a product can be increased by charging a monomer in a solid form, and a pyrrole-imidazole polyamide having any sequence can be synthesis by combining the synthesis method with a manual synthesis with an acid chloride.
专利号:US-7901664-B2 优先权日:2008-03-31 标题 :Synthesis of aluminophosphate and metalloaluminophosphate molecular sieves 发明人:CAO GUANG; AFEWORKI MOBAE; SHAH MATU J; MERTENS MACHTELD MARIA 权利人:EXXONMOBIL CHEM PATENTS INC 摘要:In a method of synthesizing an aluminophosphate or metalloaluminophosphate molecular sieve, a synthesis mixture is provided comprising water, a source of aluminum, a source of phosphorus, optionally a source of a metal other than aluminum, a tertiary amine, and an alkylating agent capable of reacting with said tertiary amine to form a quaternary ammonium compound capable of directing the synthesis of said molecular sieve. The synthesis mixture is maintained under conditions sufficient to cause the alkylating agent to react with the tertiary amine to produce the quaternary ammonium compound and to induce crystallization of the molecular sieve.
专利号:US-12281135-B2 优先权日:2019-07-25 标 题 :Synthesis of 6-azido-6-deoxy-2-n-acetyl-hexosamine-nucleoside diphosphate 发明人:HOOGENBOOM JORIN; WIJDEVEN MARIA ANTONIA; VERKADE JORGE MERIJN MATHIEU; VAN DELFT FLORIS LOUIS; VAN BERKEL SANDER SEBASTIAAN 权利人:SYNAFFIX BV 摘要:The current invention concerns methods for the synthesis of 6-azido-6-deoxy-2-N-acetyl-monosaccharide-nucleoside diphosphate, in particular 6-azido-6-deoxy-2-N-acetyl-D-galactosamine-nucleoside diphosphate or 6-azido-6-deoxy-2-N-acetyl-D-glucosamine-nucleoside diphosphate. The synthesis method according to the invention is characterized by being highly efficient and high yielding. Also part of the present invention are key intermediates of this process.
专利号:US-9765077-B2 优先权日:2015-05-29 标题:Synthesis of duocarmycin analogues 发明人:STEPHENSON MICHAEL J; HOWELL LESLEY A; SEARCEY MARK 权利人:UNIV OF EAST ANGLIA 摘要:A novel Fmoc protected duocarmycin subunit and utilization as a reagent in solid phase protein synthesis methodology. Also provided is a novel method of solid phase peptide synthesis, and in particular a method for the production of novel intermediates and novel monomeric and extended duocarmycin analogues having amino acid substituents.
专利号:US-9688644-B2 优先权日:2009-04-30 标 题 :Synthesis of Tetracyclines and intermediates thereto 发明人:MYERS ANDREW G; KUMMER DAVID A; LI DERUN; HECKER EVAN; DION AMELIE; WRIGHT PETER M 权利人:HARVARD COLLEGE 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for substituents at positions 4a, 5, 5a, and 12a of the tetracycline ring system.
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