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Advanced C-prenylated intermediates for three aromatase inhibitors, including morachalcone A, can be synthesized through a Claisen-Schmidt condensation followed by Florisil®-catalyzed [1,3]-sigmatropic rearrangement of a prenyl phenyl ether.  相似文献   

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The preparation of two new synthons, 2,5- and 2,6-dibromotryptophan esters, and their use in diastereoselective intramolecular N-acyliminium ion spirocyclization methodology for the rapid construction of spirotryprostatin A and analogues are described.  相似文献   

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We achieved the total synthesis of the histone deacetylase inhibitor spiruchostatin A, as the prelude to the preparation of a combinatorial library of its analogues. Two key reactions were an asymmetric acetate aldol reaction using a Zr-enolate and macrolactonization using the Shiina method.  相似文献   

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A total synthesis of phomactin A (1) based on a Cr(II)/Ni(II) macrocyclisation from the aldehyde vinyl iodide 11, leading to 12, followed by elaboration of the epoxyketone 16, which then undergoes spontaneous pyran-hemiacetal formation on deprotection, is described.  相似文献   

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A total synthesis of millingtonine A, a diglycosylated alkaloid, has been accomplished. Millingtonine A possesses a unique racemic tricyclic core structure not known from any other natural or synthetic source until now. The synthesis features a key bond-forming radical Ueno-Stork cyclization to form the heterocyclic core.  相似文献   

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In this paper, we report a total synthesis of a naturally occurring pyrrolo[2,3-d]pyrimidine nucleoside, mycalisine A. Our synthetic strategy uses D-xylose as the startingmaterial and Vorbrüggen glycosylation as the key step. Mycalisine A was synthesized in 11 steps with a 15% overall yield.  相似文献   

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《Tetrahedron: Asymmetry》1998,9(8):1351-1357
Synthesis of 1, a component of cryptophycin A 2 and arenastatin A 3, was achieved by applying palladium-catalyzed reductive ring opening of optically active alkenyl oxirane 13 for the construction of the vicinal stereogenic centers.  相似文献   

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A concise and straightforward 14-step total synthesis of (+/-)-salinosporamide A, based on a diastereoselective acid-catalysed intramolecular cyclisation of to the pyrrolidinone , and a regioselective reduction of the malonate derivative 8b to the aldehyde 9, is described.  相似文献   

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[reaction: see text]. A total synthesis of naamidine A is reported. Key benefits of the described pathway include its brevity, its synthetic ease, and its flexibility with respect to the preparation of analogues. Formation of the 2-aminoimidazole core is achieved by condensation of the appropriate alpha-aminoketone with cyanamide.  相似文献   

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A modified total synthesis of cystothiazole A is described. In this synthetic strategy, a one-step transformation of acylated oxazolidinone to β-ketoester has been successfully applied, thus making the synthetic route more efficient. This method may also be potentially applied in synthesis of other related β-substituted-β-methoxyl acrylates (bb-MOAs).  相似文献   

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An effective and enantioselective process for the total synthesis of (+)-brefeldin A (1) is described which starts from the dextrorotatory ketone2.  相似文献   

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A convergent synthesis of the macrocyclic core of the marine macrolide leucascandrolide A has been accomplished.  相似文献   

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Juglomycin A has been synthesized in four steps from 5-methoxy-1-naphthol.  相似文献   

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A simple stereocontrolled synthesis of salinosporamide A   总被引:1,自引:0,他引:1  
A simple and effective stereocontrolled synthesis of salinosporamide A has been developed. This process, the first synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. Salinosporamide A was of special interest as a synthetic target because of its potent in vitro cytotoxic activity against many tumor cell lines (IC(50) values of 10 nM or less).  相似文献   

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A total synthesis of the von Willebrand factor receptor antagonist sulfobacin A is described. Key steps for this short route to sulfobacin A include ruthenium-catalyzed asymmetric hydrogenation and diastereoselective electrophilic amination for the construction of the three stereogenic centers.  相似文献   

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Patellamide A was efficiently synthesized from thiazole 2 via two complementary heterocyclization approaches to form the thiazole and oxazoline rings.  相似文献   

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