- Practical synthesis of FR195752, the side chain of Micafungin, utilizing a regioselective conversion of diaryl-β-diketone to 3,5-diarylisoxazole
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The practical synthesis of FR195752, the side chain of Micafungin, was established utilizing a highly regioselective conversion of diaryl-β- diketone to 3,5-diarylisoxazole via the corresponding β-keto enamine intermediate whose disfavored regioisomer could be recycled efficiently after its hydrolysis. In addition, the related substance of FR195752 could be strictly controlled by the purification of its intermediate.
- Ohigashi, Atsushi,Kanda, Atsushi,Tsuboi, Hiroyuki,Hashimoto, Norio
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Read Online
- Preparation method of micafungin derivative side chain intermediate
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The invention provides a preparation method of a micafungin derivative side chain intermediate. The method is a preparation method of the micafungin derivative side chain intermediate, and the micafungin derivative side chain intermediate is prepared by directly taking monoterephthalate as a raw material. The process route is greatly shortened, toxic and high-pollution noble metal catalysts are prevented from being prepared and used, impurities difficult to remove are prevented from being generated due to excessive reaction, the process is simple, few equipment is occupied, operation is easy and convenient, and the method is suitable for industrial application.
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- Preparation method of high-purity micafungin intermediate
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The invention belongs to the field of drug synthesis, relates to a preparation method of a high-purity micafungin intermediate, and concretely relates to a preparation method of a micafungin intermediate compound represented by formula A-4. The synthesis method is simple to operate and high in yield, and can meet the requirements of industrial production.
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Paragraph 0028; 0029
(2020/05/30)
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- A concise synthesis of isoxazole-based side chain of Micafungin
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A concise synthesis of key isoxazole-based side chain of Micafungin, an USFDA approved anti-fungal agent, has been delineated. The route design notably involves a one pot regioselective isoxazole construction from the corresponding aryl aldehyde and alkyne intermediates.
- Rao, Pallavi,Hussain, Ismail,Rao, Venkataramanarao,Sen, Saikat,Oruganti, Srinivas
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p. 2180 - 2187
(2019/06/25)
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- Synthesis and antifungal evaluation of pentyloxyl-diphenylisoxazoloyl pneumocandins and echinocandins
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Echinocandins and pneumocandins are classes of lipocyclohexapeptides that are broad spectrum antifungal agents. They inhibit fungal specific 1,3-β-glucan synthase activity which is an essential component of the fungal cell wall. Chemical modifications of
- Singh, Sheo B.,Herath, Kithsiri,Kahn, Jennifer Nielsen,Mann, Paul,Abruzzo, George,Motyl, Mary
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p. 3253 - 3256
(2013/06/27)
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- Lipopeptide Compounds and Their Use
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The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain lipopeptide compounds comprising a cyclic peptide bearing a lipid side chain (for convenience, collectively referred to herein as “LP compounds”), which, inter alia, are antimicrobial, particularly antibacterial. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to provide an antimicrobial function, particularly an antibacterial function, and in the treatment of diseases and conditions that are mediated by microbes, particularly bacteria, that are ameliorated by the antimicrobial function, particularly an antibacterial function, including bacterial diseases, optionally in combination with another agent, for example, another antibacterial agent.
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- Novel echinocandin antifungals. Part 2: Optimization of the side chain of the natural product FR901379. Discovery of micafungin
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Further optimization of the potent antifungal activity of side chain analogs of the natural product FR901379 led to the discovery of compound 8 with an excellent, well-balanced profile. Potent compounds with reduced hemolytic potential were designed based upon a disruption of the linearity of the terphenyl lipophilic side chain. The optimized compound (8, FK463, micafungin) displayed the best balance and was selected as the clinical candidate.
- Tomishima, Masaki,Ohki, Hidenori,Yamada, Akira,Maki, Katsuyuki,Ikeda, Fumiaki
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p. 2886 - 2890
(2008/12/23)
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- NEW PROCESS
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The present invention relates to a process for preparing a pharmaceutical starting compound compound by hydrolyzing a compound of the general formula (II): Wherein R1 is protected carboxy, R2 is lower alkoxy or higher alkoxy, A1
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