CAS: 527-75-3; (3R,4S,5S,6R,7R,9R,11R,12S,13R,14R)-6-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-Hydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-14-Ethyl-7,12-Dihydroxy-4-(((2R,4R,5S,6S)-5-Hydroxy-4-Methoxy-4,6-Dimethyltetrahydro-2H-Pyran-2-yl)Oxy)-3,5,7,9,11,13-Hexamethyloxacyclotetradecane-2,10-Dione

上下游产品

CAS号188786-14-3 (2R,3R,4R,6R,7S... | CAS号188786-05-2 (2S,3R,4R,6R,8R...

📜(2R,3R,4R,6R,7S,8S,9S,10S,11R)-11-[(Benzyloxy)Methoxy]-4-[(Tert-Butyldimethylsilyl)Oxy]-3-[(4-Methoxybenzyl)Oxy]-2,4,6,8,10-Pentamethyl-7,9-{[(R)-2,4,6-Trimethylbenzylidene]Dioxy}Tridecanal置于palladium On Activated Charcoal 吡啶,盐酸,甲醇,4-二甲氨基吡啶,Disodium Hydrogenphosphate,Potassium Dihydrogenphosphate,Oil Scarlet,3 A Molecular Sieve,4 A Molecular Sieve,三氟化硼乙醚,四丁基氟化铵,水,氢气,Silver Trifluoromethanesulfonate,Copper(II) Bis(Trifluoromethanesulfonate),戴斯-马丁氧化剂,臭氧,溶剂黄146,三乙胺,间氯过氧苯甲酸,2,3-二氯-5,6-二氰基-1,4-苯醌,Copper(II) Oxide体系中,用 四氢呋喃,甲醇,二氯甲烷,水,甲苯,乙腈 作为反应溶剂,化学反应 110.25H,反应生成 红霉素b
参考文献:全合成红霉素b
标题:全合成红霉素b
摘要:我们报告了使用两种不同策略进行最终比赛时红霉素b首次完全合成的详细信息.这些方法中的第一种遵循经典方法,其中将去氨胺和可乐宁残基顺序连接到大环内酯上,该内酯是通过癸二酸衍生物的环化形成的,得到双糖基化大环内酯中间体,该中间体被转化为红霉素b.第二种策略的特征是一种非生物方法,其中将带有去氨胺残基的癸二酸环化,反应生成单糖基化的大环内酯,然后通过一系列步骤将其转化为红霉素b,所述步骤包括重新官能化和糖基化以引入可乐定.通过从头合成来制备双糖基化的癸二酸的尝试是失败的.关键癸二酸中间体的合成特征在于含有c(3)-c(10)的呋喃的氧化转化,以提供二氧杂双环[3.3.1]壬烯酮,该模板用作在c(6)上建立立体中心的模板)和c(8).立体选择性羟醛反应用于建立c(11)-C(15)段,并进行立体选择性交联以引入包含c(1)-C(2)的丙酸酯亚基.
DOI:10.1016/j.Tet.2007.02.044

专利信息

专利号:US-2008044860-A1
优先权日:2003-11-28
标题 :Polyketides and Their Synthesis
发明人：GAISSER SABINE; HAYDOCK STEPHEN FREDERICK; LEADLAY PETER FRANCIS; MCARTHUR HAMISH ALASTAIR IRVIN
权利人:GAISSER SABINE; HAYDOCK STEPHEN FREDERICK; LEADLAY PETER FRANCIS; MCARTHUR HAMISH ALASTAIR IRVIN
摘要:Macrolides particularly erythromycins and azithromycins, having O-mycaminosyl or O-angolosaminyl groups, particularly at the 5 -position, are produced using a gene cassette comprising a combination of genes which, in an appropriate strain background, are able to direct the synthesis of mycaminose or angolosamine and to direct its subsequent transfer to an aglycone or pseudoaglycone. Synthetic genes may comprise one or more of angMIII, angMI, angB, angAI, angAII, angorf14, angorf4, tylMIII, tylMI, tylB, tylAI, tylAII, eryCVI, spnO, eryBVI, eryK, tyl Ia and ery G. Glycosyltransfer genes may comprise one or more of eryCIII, tylMII, angMII, desVII, eryBV, spnP and midI.

专利号:WO-2004075874-A1
优先权日:2003-02-28
标题 :Method for treatment and prevention of acute and chronic pseudomonas aeruginosa airway infections with inhalable macrolides
发明人：MENEKSE OKTAY
权利人:ANBICS PATENTS LICENCES AG; MENEKSE OKTAY
摘要:Macrolides, in particular azalides such as azithromycin, are suited for the treatment or prevention of acute or chronic P. aeruginosa infections of the airways by inhala­tion. The mechanism of action is the inhibition of the quo­rum sensing of P. aeruginosa, in particular the impediment of the las and rhl quorum sensing systems synthesis and the impediment of the synthesis of the autoinducers N-[3-oxodo­1o decanoyl]-L-homoserine lactone and N-butyrylhomoserine lac­tone. This allows for inhalation treatments of P. aerugi-nosa infections at non-inhibiting concentrations of the macrolide.

专利号:US-6004787-A
优先权日:1991-01-17
标题:Method of directing biosynthesis of specific polyketides
发明人：KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
权利人:ABBOTT LAB
摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccarharopolyspora or Streptomyces.

专利号:US-5912331-A
优先权日:1991-03-15
标题:Process for the preparation of 9-deoxo-9(Z)-hydroxyiminoerythromycin A
发明人：WILKENING ROBERT R
权利人:MERCK & CO INC
摘要:A method is presented for isomerizing the E-isomer of 9-Deoxo-9-hydroximinoerythromycin A to its corresponding Z-isomer. The Z-isomer is useful as an antibiotic and as an intermediate for the synthesis of other macrolide antibiotics.

专利号:WO-9313663-A1
优先权日:1992-01-17
标 题:Method of directing biosynthesis of specific polyketides
发明人：KATZ LEONARD; DONADIO STEFANO; MCALPINE JAMES B
权利人:ABBOTT LAB
摘要:A method to produce novel polyketide structures by designing and introducing specified changes in the DNA governing the synthesis of the polyketide is disclosed. The biosynthesis of specific polyketide analogs is accomplished by genetic manipulation of a polyketide-producing microorganism by isolating a polyketide biosynthetic gene-containing DNA sequence, identifying enzymatic activities associated within the DNA sequence, introducing one or more specified changes into the DNA sequence which codes for one of the enzymatic activities which results in an altered DNA sequence, introducing the altered DNA sequence into the polyketide-producing microorganism to replace the original sequence, growing a culture of the altered microorganism under conditions suitable for the formation of the specific polyketide analog, and isolating the specific polyketide analog from the culture. The method is most useful when the segment of the chromosome modified is involved in an enzymatic activity associated with polyketide biosynthesis, particularly for manipulating polyketide synthase genes from Saccharapolyspora or Streptomyces.

专利号:US-9693999-B2
优先权日:2011-01-26
标题:Small molecule RNase inhibitors and methods of use
发明人：DUNMAN PAUL M; OLSON PATRICK D; CHILDERS WAYNE
权利人:UNIV ROCHESTER; UNIV NEBRASKA; Temple University—Of the Commonwealth System of Higher Education
摘要:Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease. Also described herein are methods of identifying compounds for treating or preventing a microbial infection.