- PANTETHEINE DERIVATIVES AND USES THEREOF
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The present disclosure relates to compounds of Formula (I), (II), or (II'): (I), (II), (II'), and pharmaceutically acceptable salts or solvates thereof. The present disclosure also relates to pharmaceutical compositions comprising the compounds and therapeutic and diagnostic uses of the compounds and pharmaceutical compositions.
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Paragraph 2121
(2020/06/19)
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- Isobenzofurans as Synthetic Intermediates: Synthesis and Biological Activity of 8-epi-(–)-Ajudazol B
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Ajudazol B is a polyketide secondary metabolite, isolated from the myxobacterium Chondromyces crocatus, that exhibits potent biological activity. Herein, we report a convergent total synthesis of 8-epi-(–)-ajudazol B. The key step is a regio-selective alk
- Adair, Liam,Egan, Ben A.,Pearson, Colin M.,Lopez-Gonzalez, Ricardo,Kuchar, Michal,Mendoza-Mendoza, Artemio,Prunet, Jo?lle,Marquez, Rodolfo
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supporting information
p. 6661 - 6672
(2020/10/15)
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- Total Synthesis of Ajudazol A by a Modular Oxazole Diversification Strategy
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The total synthesis of the potent respiratory chain inhibitor ajudazol A was accomplished by a concise strategy in 17 steps (longest linear sequence). The modular approach was based on a direct oxazole functionalization strategy involving a halogen dance
- Essig, Sebastian,G?lz, Jan Philipp,Menche, Dirk,Von Schwarzenberg, Karin,Wollnitzke, Philipp
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supporting information
(2020/09/02)
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- Full stereochemical determination of ajudazols a and b by bioinformatics gene cluster analysis and total synthesis of ajudazol B by an asymmetric ortholithiation strategy
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The stereochemical determination of the potent respiratory chain inhibitors ajudazols A and B and the total synthesis of ajudazol B are reported. Configurational assignment was exclusively based on biosynthetic gene cluster analysis of both ketoreductase
- Essig, Sebastian,Bretzke, Sebastian,Müller, Rolf,Menche, Dirk
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supporting information
p. 19362 - 19365
(2013/02/21)
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- Iridium-catalyzed asymmetric hydrogenation of vinyl ethers
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A carbene-oxazoline catalyst 1 proved to be an effective catalyst for reduction of an enol ether that the literature suggested could not be hydrogenated effectively by P,N-Ir catalysts. Thus, a series of ester and alcohol substrates were hydrogenated using catalyst 1. Good to excellent enantioselectivities and high conversions were obtained.
- Zhu, Ye,Burgess, Kevin
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supporting information; experimental part
p. 979 - 983
(2009/05/30)
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- Synthesis of the eastern portion of ajudazol a based on stille coupling and double acetylene carbocupration
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(Chemical Equation Presented) A strategy for the synthesis of ajudazol A, an unusual, pharmacologically active metabolite from myxobacteria, based on the Stille cross-coupling of a 2-stannyl-oxazole with a vinyl iodide unit is described; the vinyl halide unit containing a (Z,Z)-diene was prepared in one pot by the double acetylene carbocupration of a functionalized alkyl cuprate followed by trapping with 2,3-dibromopropene.
- Krebs, Oliver,Taylor, Richard J. K.
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p. 1063 - 1066
(2007/10/03)
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- Haloacetylated Enol Ethers. 8 [12]. Reaction of β-Alkoxyvinyl Trihalomethyl Ketones with Guanidine Hydrochloride. Synthesis of 4-Trihalomethyl-2-Aminopyrimidines
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In this work the results of the reaction of β-alkoxyvinyl trihalomethyl ketones 1, 2a-e, with guanidine hydrochloride are reported. Depending on the ketone 1 or 2 and the conditions under which the reactions were carried out, 4-trihalomethyl-2-amino pyrimidines, β-alkoxyvinyl carboxylic acids, or β-acetal carboxylic esters were obtained.
- Zanatta, Nilo,Cortelini, Maria De F. M.,Carpes, Marcos J. S.,Bonacorso, Helio G.,Martins, Marcos A. P.
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p. 509 - 513
(2007/10/03)
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- VINYL ETHER HYDROLYSIS. 30. EFFECT OF β-CARBOXY AND β-CARBOMETHOXY SUBSTITUTION
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Rates of hydrolysis of the vinyl ether functional groups of (Z)- and (E)-β-methoxyacrylic acid and (Z)- and (E)-β-methoxymethacrylic acid and their methyl esters were measured in aqueous perchloric acid solution.Additional rate measurements were also made for one substrate, (Z)-β-methoxymethacrylic acid, in buffer solutions down to pH 7, and a rate profile was constructed.The results show that the β-carboxy and β-carbomethoxy substituents produce strong rate retardations, ranging from 2000- to 25 000-fold, for both Z- and E-isomers in both the acrylic and methacrylic acid series.The rate profile for (Z)-β-methoxymethacrylic acid indicates that ionization of this substrate to the carboxylate ion form raises the rate of hydrolysis by a factor of 240.It is argued that this difference in reactivity of ionized and non-ionized forms of the substrate is due to conjugative and inductive effects of the substituents, rather than β-lactone formation as suggested in an earlier observation of the same phenomenon in a different system.
- Kresge, A. J.,Ubysz, D.
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p. 316 - 322
(2007/10/02)
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