CAS: 873857-62-6; (2R,3S,4S,5S,6R)-6-(((3E,5E,8S,9E,11S,12R,13E,15E,18S)-12-(((2R,3S,4R,5S)-3,4-Dihydroxy-5-(Isobutyryloxy)-6,6-Dimethyltetrahydro-2H-Pyran-2-yl)Oxy)-11-Ethyl-8-Hydroxy-18-((R)-1-Hydroxyethyl)-9,13,15-Trimethyl-2-Oxooxacyclooctadeca-3,5,9,13,15-Pentaen-3-Yl

Didechlorotiacumicin B 在 Halogenase Tiam,Fad,还原型辅酶ⅰ,Sodium Chloride体系中,反应 0.5H,获得 Fidaxomicin
参考文献:一种简便易行的双氯硫霉素b与芳香族化合物的碘化方法
标题:一种简便易行的双氯硫霉素b与芳香族化合物的碘化方法
摘要:Tiacumicin B(也称为 Fidaxomicin 或 Difimicin)是一种市售的 18 元大环内酯抗生素,用于治疗艰难梭菌感染.Tiacumicin B 的结构特征是芳环上被两个氯原子取代,由卤化酶 Tiam 安装.在研究 Tiam 的卤化物相容性期间,发现了一种简便,非酶促的双氯硫霉素 B 碘化方法,需要 Nai,酸和空气在室温下进行碘化.该方法也适用于其他 9 种具有富电子位点的芳香族底物用于碘化.
Doi:10.1007/S11426-021-1072-6

专利信息

专利号:US-2023399688-A1
优先权日:2015-08-20
标 题 :Compositions and multiplexed systems for coupled cell-free transcription-translation and protein synthesis and methods for using them
发明人：CULLER STEPHANIE; CHEN IHSIUNG BRANDON; PHARKYA PRITI; VAN DIEN STEVE; BARTON NELSON
权利人:GENOMATICA INC
摘要:In alternative embodiments, provided herein are transcription/translation (TX-TL) systems and methods of using them for use as rapid prototyping platforms for the synthesis, modification and identification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites, from biosynthetic gene cluster pipelines. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the combinatorial biosynthesis of natural products (NPs), natural product analogs (NPAs) and secondary metabolites. In alternative embodiments, exemplary TX-TL systems as provided herein are used for the rapid prototyping of complex biosynthetic pathways as a way to rapidly assess combinatorial and biosynthetic designs before moving to cellular hosts. In alternative embodiments, these exemplary TX-TL systems are multiplexed for high-throughput (HT) automation and for prototyping engineered platforms for the synthesis or modification of natural products (NPs), and natural product analogs (NPAs) and secondary metabolites analogs.

专利号:US-12344632-B2
优先权日:2015-12-21
标 题:System and method for solution phase gap peptide synthesis
发明人：LI GUIGEN; SEIFERT COLE
权利人:UNIV TEXAS TECH SYSTEM
摘要:Disclosed is a system and method for Fmoc/tBu solution-phase peptide synthesis including the development of a new benzyl-type GAP protecting group, and related uses thereto. This novel GAP protecting group is utilized in place of a polymer support, facilitating C to N Fmoc peptide synthesis without chromatography, recrystallization, or polymer supports. The GAP group can be added and removed in high yield.

专利号:US-11827660-B2
优先权日:2019-02-01
标题 :Synthesis strategy for gap protecting group
发明人：SEIFERT COLE
权利人:SEDERMA SA
摘要:The present invention relates to a novel synthesis method to form particular molecules. These molecules have multiple uses, most notably in the field of protecting groups used throughout organic and synthetic chemistry. The disclosed method is safer, more cost- and time-effective, and more amenable to large scale production than those currently known in the art. The protecting groups synthesized are useful in GAP peptide synthesis.

专利号:US-2024207302-A1
优先权日:2021-04-01
标 题 :Antiviral compounds, methods for the manufacturing of compounds, antiviral pharmaceutical composition, use of the compounds and method for the oral treatment of coronavirus infection and related diseases thereof
发明人：CALIXTO JOãO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
权利人:CALIXTO JOAO BATISTA; RABI NALLAR JAIME ALBERTO; LOPES E SOUZA THIAGO MORENO
摘要:The present invention relates to antiviral compounds selected from cytokinins, their nucleosides and nucleotide analogs, and their prodrugs as inhibitors of viral RNA synthesis, or their salts, solvates, derivatives, or even combinations of aforementioned compounds, for prophylactic treatment, curative (therapeutic) or mitigative coronavirus infection, represented by human and veterinary coronavirus, SARS-COV-2 and MHIV, and for the treatment of individuals potentially exposed to COVID-19. The present invention also comprises the methods for the manufacturing of such compounds, the antiviral pharmaceutical composition containing the compounds of the invention, as well as the use of the compounds, combinations of compounds, and method for the prophylactic, curative (therapeutic) or mitigative treatment of coronavirus infection, represented by coronavirus, in especial SARS-COV-2 and of patients with COVID-19, individual infected with SARS-COV-2 or potentially exposed to this virus. The antiviral activity of the compounds of this invention against SARS-COV-2 was greatly enhanced by inhibiting the 3′-5′-exonuclease. Synergistic results of the compounds according to the present invention were obtained from the combination with repurposed drugs.

专利号:US-2022403431-A1
优先权日:2020-02-14
标 题 :Glycominimized bacterial host cells
发明人：BEAUPREZ JOERI; DE MAESENEIRE SOFIA; SNOECK NICO
权利人:INBIOSE NV
摘要:This disclosure is in the technical field of synthetic biology and metabolic engineering. The disclosure provides engineered viable bacteria having a reduced or abolished synthesis of poly-N-acetyl-glucosamine (PNAG), Enterobacterial Common Antigen (ECA), cellulose, colanic acid, core oligosaccharides, Osmoregulated Periplasmic Glucans and Glucosylglycerol (O), glycan, and trebalose. The disclosure further provides methods for the production of bioproduct by the viable bacteria and uses thereof. Furthermore, the disclosure is in the technical field of fermentation of metabolically engineered microorganisms producing bioproduct.

专利号:US-10065924-B2
优先权日:2014-07-22
标 题 :Preparation and biological evaluation of viridicatumtoxin analogs
发明人：NICOLAOU KYRIACOS C; HALE CHRISTOPHER R H; NILEWSKI CHRISTIAN; IOANNIDOU HERAKLIDIA; EL MARROUNI ABDELLATIF
权利人:UNIV RICE WILLIAM M
摘要:In one aspect, the present invention provides novel derivatives of viridicatumtoxin of the formula wherein the variables are as defined herein. The application also provides compositions, methods of treatment, and methods of synthesis thereof.