- EFFICIENT AND SCALABLE SYSTHESIS OF 2-(1'H-INDOLE-3'-CARBONYL)-THIAZOLE-4-CARBOXYLIC ACID METHYL ESTER AND ITS STRUCTURAL ANALOGS
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Methods of synthesizing 2-(1'H-indole-3'-carbonyl)-thiazole-4-carboxylic acid methyl ester (ITE) and structural analogs thereof. The methods include condensation reactions or condensation and oxidation reactions to form the thiazoline or thiazole moiety of ITE or its structural analogs.
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Page/Page column 25
(2016/06/01)
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- Assembly of the nosiheptide A-ring: A fruitful lesson
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The synthesis of a 28-membered thiopeptide macrocycle is described. Key steps are mild aza-Wittig thiazole ring closures, a scandium(III)-mediated regioselective ester hydrolysis, and a highly efficient macrolactam formation with its 3-hydroxypyridine nucleus orthogonally protected. Georg Thieme Verlag Stuttgart, New York.
- Lu, Jin-Yong,Riedrich, Matthias,Wojtas, K.Philip,Arndt, Hans-Dieter
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supporting information
p. 1300 - 1311
(2013/07/04)
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- PROPYL 3-BROMO-2-OXOPROPIONATE AND DERIVATIVES AS NOVEL ANTICANCER AGENTS
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The present invention is directed to compositions that inhibit glycolysis, preferentially in cancer. Specifically, the anticancer compositions comprise 3-halo-2-oxopropionate and its derivatives, such as ester derivatives. However, in specific embodiments, the anticancer composition is sodium 3-halo-2-oxopropionate, such as sodium 3-bromo-2--oxopropionate and a stabilizing agent, such as carbonic acid. In particular embodiments, the compositions of the present invention further comprise a metabolic intermediate for normal cells to utilize in a pathway for an alternate energy source, thereby providing protection to normal cells. In other embodiments, the 3-halo-2-oxopropionate or its ester derivative is used in combination with an additional cancer therapy, such as radiation and/or a drug.
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Page/Page column 58
(2008/06/13)
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- Total synthesis and absolute configuration of radiosumin, a strong trypsin inhibitor from the blue-green alga Plectonema radiosum
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Radiosumin (1), a strong trypsin inhibitory dipeptide isolated from the freshwater blue-green alga Plectonema radiosum (NIES-515), was synthesized for the first time by use of the hetero Diels-Alder reaction, the Horner-Wadsworth-Emmons reaction, the Corey-Winter reaction, regioselective hydrogenation, and reduction with zinc and formic acid as key steps, which unambiguously determined the absolute configuration of the structurally unique and biologically intriguing aquatic natural product (1).
- Noguchi, Hirohide,Aoyama, Toyohiko,Shioiri, Takayuki
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p. 471 - 504
(2007/10/03)
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