- Therapeutic and diagnostic ligand systems comprising transport molecule binding properties and medicaments containing the same
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The invention relates to transport molecule binding ligand compounds which comprise a therapeutically and/or diagnostically active substance and a carrier molecule-affine substance with a high association constant to the carrier molecule. The invention also relates to medicaments containing these ligand compounds and to diagnostic kits.
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- Asymmetric synthesis of a lignan lactone from a meso anhydride
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The synthesis of a meso-2,3-dibenzylbutanedioic acid anhydride is given. Reaction of this with (+)-α-methylbenzylamide proceeds diastereoselectively to give a butanedioic acid monoamide which is converted into an enantiomerically enriched cis-2,3-dibenzyl
- Ward, Robert S.,Pelter, Andrew,Edwards, Mark I.,Gilmore, Jeremy
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p. 12799 - 12814
(2007/10/03)
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- New synthetic route to butanolide lignans by a ruthenium complex catalyzed hydrogenation of the corresponding Stobbe's fulgenic acids
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A new two-step total synthesis of butanolide lignans (or dibenzylbutyrolactone lignans) is described, which affords the title compounds in good yield and with a very short work-up time. It involves a ruthenium carbonyl hydride complex-catalyzed hydrogenation of the corresponding dibenzylidene succinic acids (fulgenic acids). Since the catalytic hydrogenation (second step) is a total yielding process, the overall yield determining step is the preparation of the fulgenic acid intermediates by the Stobbe condensation (first step), which has consequently been revised to improve many details. This simple process moreover allows hexadeuterated butanolide lignans to be readily obtained for isotopic dilution mass spectral measurements. The syntheses of a selection of lignans, namely enterolactone, matairesinol, hinokinin, dimethylmatairesinol and cordigerine, are described to illustrate the whole procedure.
- Bambagiotti-Alberti, Massimo,Coran, Silvia A.,Vincieri, Franco F.,Mulinacci, Nadia,Pieraccini, Giuseppe M.L.
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p. 2185 - 2196
(2007/10/02)
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- Rotamers and Isomers in the Fulgide Series. Part 1. Stereochemistry and Conformational Analysis of Bis-(3,4-dimethoxybenzylidene)succinic Anhydrides by X-Ray Crystallography and Molecular Mechanics
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Conformational analysis of bis-(3,4-dimethoxybenzylidene)succinic anhydride suggests that in addition to a Z,Z-isomer, the E,E-isomer of this diarylfulgide occurs as three distinct relatively freely interconvertible chiral rotamers and their enantiomers.T
- Boeyens, Jan C. A.,Denner, Louis,Perold, Guido W.
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p. 1749 - 1758
(2007/10/02)
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- Nucleophilic reactivity of dehydrodiferulic acid bislactone
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Despite reports to the contrary, dehydrodiferulic acid bislactone can readily undergo nucleophilic attack.Silylation affords the disilyl ether-disilyl ester of the corresponding bismethylenesuccinic acid.Slow dissolution of the bislactone in sodium hydrogen carbonate solution affords this parent diacid, characterised as its mono- and dimethyl esters, and by its methylation to bisveratrylidenesuccinic acid, whose anhydride on aerial oxidation yields 6,7-dimethoxy-1-(3',4'-dimethoxyphenyl)naphthalene-2,3-dicarboxylic anhydride.
- Boshoff, Philip R.,Perold, Guido W.
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p. 735 - 745
(2007/10/02)
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- Synthesis of 3,4-Bis-dihydro-2(3H)-furanones and 2,3-Bis(m- or p-substituted-benzyl)-butane-1,4-diols.
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Stobbe condensation of appropriately substituted aromatic aldehydes with diethyl or dimethyl succinate in the presence of sodium methoxide yields the required starting materials for the synthesis of the title compounds.The diacids (1-4) and half acid-half
- Neelima,Bhaduri, A. P.
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p. 209 - 215
(2007/10/02)
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