CAS: 62013-04-1; (1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-9-(((2S,3R,4S,6R)-4-(Dimethylamino)-3-Hydroxy-6-Methyltetrahydro-2H-Pyran-2-yl)Oxy)-3-Ethyl-2,10-Dihydroxy-7-(((2R,4R,5S,6S)-5-Hydroxy-4-Methoxy-4,6-Dimethyltetrahydro-2H-Pyran-2-yl)Oxy)-15-((2-Methoxyethoxy)Meth

(2-甲氧基乙氧基)乙醛缩二甲醇 在 水,对甲苯磺酸体系中,用 乙腈作为反应溶剂,反应 18.0H,获得 Dirithromycin
参考文献:Generation Of Stable Synthetic Equivalents Of Unstable α-Alkoxyacetaldehydes: An Improved Preparation Of Dirithromycin
标题:Generation Of Stable Synthetic Equivalents Of Unstable α-Alkoxyacetaldehydes: An Improved Preparation Of Dirithromycin
摘要:描述的是α-烷氧基乙醛的半缩醛的原位制备. 半缩醛是通过缩醛前体在乙腈水溶液中水解生成的.这些半缩醛作为稳定的醛等价物,从而避免了不稳定的α-烷氧基醛的产生和分离. 2-甲氧基乙氧基乙醛的半缩醛可有效且高效地制备地红霉素 (Ly237216).
Doi:10.1055/S-1993-26006

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2024197774-A1
优先权日:2021-04-16
标 题:Synthesis of Antimicrobial PVP-coated Bismuth Nanoparticles
发明人：LOPEZ-RIBOT JOSE; VAZQUEZ-MUNOZ ROBERTO
权利人:UNIV TEXAS
摘要:Described herein is a facile, fast, and economical method for the synthesis of BAL-mediated PVP-BiNPs, using basic laboratory instruments and reagents readily available in most laboratories.

专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人：DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).

专利号:US-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

专利号:WO-2015014261-A1
优先权日:2013-07-30
标 题:Macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof
发明人：SHEN SHUNYI; CHEN DAIJIE; GE HAN; ZHANG ZHIHONG; REN YANSONG; LI ZHONGLEI; FAN QIANYONG; ZHANG YUN; XU YIJUN; LI DAN; LI JIAN
权利人:SHANGHAI INSITITUTE OF PHARMACEUTICAL INDUSTRY; CHINA STATE INST PHARM IND
摘要:The present invention discloses a macrolide compound or salt thereof, synthesis method, pharmaceutical composition, and application thereof. The present invention provides a method for preparing a macrolide compound 1, a macrolide compound 1', or a salt thereof; also provided are a macrolide compound 2, macrolide compound 2', or salt thereof, a pharmaceutical composition containing said compound or salt, and the application thereof in the preparation of a pharmaceutical for inhibiting methicillin-resistant Staphylococcus aureus. When one or more of the macrolide compound 2, the macrolide compound 2', the macrolide compound 2 salt, and the macrolide compound 2' salt of the present invention is used together with a β-lactam antibiotic, the inhibiting effect of the β-lactam antibiotic on methicillin-resistant Staphylococcus aureus is significantly increased. This is a new class of potentiator having a good potentiating effect in vitro, alleviating methicillin-resistant Staphylococcus aureus resistance to β-lactam antibiotics, and having good prospects for market development.