CAS: 760981-83-7; Solithromycin

上下游产品

(11-N-(4-Azidobutyl)-5-(2’-Benzoyldesosaminyl)-3-Oxo-2-Fluoro-6-O-Methylerythronolide A,11,12-Cyclic Carbamate)
[(2R,3S,7R,9R,10R,11S,12S,13R)-10-[(2S,3R,4S,6R)-3-Benzoyloxy-4-(Dimethylamino)-6-Methyloxan-2-Yl]Oxy-12-[(2R,4R,5S,6S)-5-Benzoyloxy-4-Methoxy-4,6-Dimethyloxan-2-Yl]Oxy-2-Ethyl-9-Methoxy-3,5,7,9,11,13-Hexamethyl-6,14-Dioxo-1-Oxacyclotetradec-4-En-3-Yl] Imidazole-1-Carboxylate
Clarithromycin Dibenzoate 484670-64-6
[(2S,3R,4S,6R)-4-(Dimethylamino)-2-[[(1R,2R,5R,6S,7S,8R,9R,11R,13R,14R)-2-Ethyl-6-Hydroxy-9-Methoxy-1,5,7,9,11,13-Hexamethyl-4,12,16-Trioxo-3,15,17-Trioxabicyclo[12.3.0]Heptadecan-8-Yl]Oxy]-6-Methyloxan-3-Yl] Benzoate 875475-90-4
[(2S,3R,4S,6R)-4-(Dimethylamino)-2-[[(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-14-Ethyl-4,12,13-Trihydroxy-7-Methoxy-3,5,7,9,11,13-Hexamethyl-2,10-Dioxo-Oxacyclotetradec-6-Yl]Oxy]-6-Methyloxan-3-Yl] Benzoate 190839-61-3
克拉霉素 Clarithromycin 81103-11-9

📜(R)-3-((Tert-Butyldimethylsilyl)Oxy)Pentan-2-One置于二氯二茂钛,Lithium (1S,2R)-1-Phenyl-2-(Pyrrolidin-1-yl)-1-Propanolate,Potassium Tert-Butylate,四丁基氟化铵,咪唑盐酸盐,戴斯-马丁氧化剂,1,8-二氮杂双环[5.4.0]十一碳-7-烯,N-氟代双苯磺酰胺,环戊基溴化镁体系中,用 氯苯 作为反应溶剂,化学反应生成 索利霉素
参考文献:发现新型大环内酯类抗生素的平台
标题:发现新型大环内酯类抗生素的平台
摘要:结构复杂的发酵产物的化学修饰(一种称为半合成的过程)一直是发现和制造用于治疗各种传染病的抗生素的重要工具.然而,以这种方式获得的许多治疗方法不再有效,因为细菌对这些化合物已经产生了耐药性.在这里,我们提出了一种实用的,全合成的大环内酯类抗生素的路线,通过简单化学结构单元的聚合组装,能够合成传统半合成方法无法获得的多种结构.使用我们的聚合方法已合成了 300 多种新的大环内酯类抗生素候选药物以及临床候选索利霉素.对这些化合物针对一组病原菌的评估表明,这些结构中的大多数具有抗生素活性,其中一些对当前使用的对大环内酯类药物具有抗性的菌株有效.我们在此描述的化学过程为发现新的大环内酯类抗生素提供了一个平台,也可以作为其制造的基础.
DOI:10.1038/nature17967

专利信息

专利号:US-9982005-B2
优先权日:2013-04-04
标 题 :Macrolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.

专利号:US-11466046-B2
优先权日:2014-10-08
标题 :14-membered ketolides and methods of their preparation and use
发明人：MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.

专利号:US-11008358-B2
优先权日:2015-03-25
标题:Synthesis of desosamines
发明人：MYERS ANDREW G; ZHANG ZIYANG
权利人:HARVARD COLLEGE
摘要:The present invention provides desosamine and mycaminose analogs and nitro sugars and methods for their preparation. The invention also provides methods of cyclizing a compound of Formula (A′) with glyoxal to give a nitro sugar of Formula (B). Methods for the preparation of compound of Formula (D′) are provided comprising cyclization of a nitro alcohol to give a nitro sugar and reduction and alkylation of the nitro sugar to give a desosamine, mycaminose, or an analog thereof.

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-10472663-B2
优先权日:2015-01-21
标 题:Procedure for the rapid determination of bacterial susceptibility to antibiotics that inhibit protein synthesis
发明人：FERNÃ?NDEZ GARCÃ?A JOSÉ LUIS; GOSÃ?LVEZ BERENGUER JAIME; BOU ARÉVALO GERMÃ?N; TAMAYO NOVAS MARIA; SANTISO BRANDARIZ REBECA; OTERO FARIÑA FÃ?TIMA MARÃ?A
权利人:ABM TECH LLC
摘要:The present invention relates to a method for the rapid evaluation of bacterial susceptibility or non-susceptibility of bacteria to antibiotics that inhibit protein synthesis. The rationale is to identify bacterial responses that depend or are influenced by protein synthesis. If this response is prevented or reduced by the antibiotic that inhibits the protein synthesis, the bacteria are susceptible to this antibiotic. Otherwise, if the response keeps similar despite the incubation with the antibiotic, the bacteria are not susceptible or resistant to this antibiotic. These responses could be determined at the DNA lev-el, cell wall level, morphological level or any other experimental approach, including metabolic, bio-chemical, physiological or genetic processes.

专利号:US-2024277799-A1
优先权日:2023-02-17
标题 :Translational Activators, Including Methods of Discovery and Uses Thereof
发明人：BARNA MARIA; LANTZ TRAVIS
权利人:UNIV LELAND STANFORD JUNIOR
摘要:Translational activators are disclosed along with uses thereof and methods to discover translational activators. Many embodiments provide methods to treat diseases and disorders caused by global downregulation of protein synthesis, including (but not limited to) ribosomopathies and neurodegenerative disorders. Certain embodiments are directed to uses of translational activators for the manufacture of medicaments to treat diseases and disorders caused by global downregulation of protein synthesis, and further embodiments are directed to methods of discovering translational activators.