CAS: 10425-71-5; 3,5-Dinitropyridin-4(1H)-One

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CAS号626-64-2 4-羟基吡啶 | CAS号5435-54-1 4-羟基-3-硝基吡啶 | CAS号31872-58-9 4-Pyridinol,3,5... | CAS号10425-70-4 4-氯-3,5-二硝基吡啶

📜4-羟基吡啶置于硫酸,硝酸体系中,化学反应 26.0H,以55%的收率获得3,5-二硝基吡啶-4-醇
参考文献:路易斯酸性硼烷,路易斯碱和平衡常数:定量路易斯酸度/碱度标度的可靠支架
标题:路易斯酸性硼烷,路易斯碱和平衡常数:定量路易斯酸度/碱度标度的可靠支架
摘要:基于三芳基硼烷与各种以 O,N,S 和 P 为中心的路易斯碱在二氯甲烷中反应的 90 个实验平衡常数,开发了针对以硼为中心的路易斯酸的定量路易斯酸度/碱度标度. 20oc.使用线性自由能关系 Log K B = La B + Lb B进行分析,可以通过两个描述符(一个用于路易斯酸度 ( La B ))的总和来计算任何类型的硼烷/路易斯碱组合的平衡常数k B.一个用于路易斯碱度(lb B).所得的路易斯酸度/碱度标度与固定的参考酸/碱无关,并且对于各种类型的三价硼中心路易斯酸有效.事实证明,新开发的路易斯酸度/碱度标度可以通过与量子化学计算或常见的物理有机描述符和已知热力学数据(δ H )的线性关系轻松扩展.此外,该实验平台可用于硼烷催化反应的合理发展.
Doi:10.1002/chem.202003916

专利信息

专利号:US-2006287520-A1
优先权日:2005-05-16
标 题 :Synthesis of salinosporamide A and analogues thereof
发明人：DANISHEFSKY SAMUEL J; ENDO ATSUSHI
权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI
摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.

专利号:US-7910623-B2
优先权日:2005-07-22
标 题 :Synthesis of scabronines and analogues thereof
发明人：DANISHEFSKY SAMUEL J; WATERS STEPHEN P
权利人:SLOAN KETTERING INST CANCER
摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.

专利号:US-2009221568-A1
优先权日:2005-11-04
标题:Synthesis of Inhibitors of FtsZ
发明人：SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY
摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.

专利号:US-8486921-B2
优先权日:2006-04-07
标 题:Synthesis of tetracyclines and analogues thereof
发明人：MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU
权利人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU; 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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.

专利号:US-7902196-B2
优先权日:2005-03-17
标 题 :Synthesis of avrainvillamide, strephacidin B, and analogues thereof
发明人：MYERS ANDREW G; HERZON SETH B; WULFF JEREMY EARLE; SIEGRIST ROMAIN; SVENDA JAKUB; ZAJAC MATTHEW ALLEN
权利人:HARVARD COLLEGE
摘要:The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection.

专利号:US-9193665-B2
优先权日:2013-05-27
标题 :Synthesis of galanal compounds and analogues thereof
发明人：CHEIN RONG-JIE
权利人:ACADEMIA SINICA
摘要:The present disclosure provides methods of preparing glucagon-like peptide-1 (GLP-1) receptor modulators, such as compounds of Formula (II) or (VI), or intermediates thereof. The compounds that may be prepared by the described methods are useful for regulating blood glucose levels and/or treating a disease mediated by a GLP-1 receptor (e.g., diabetes).