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We explore the adaptability at a protein-DNA interface using phage display to re-engineer a homeodomain to specifically recognize a chemically synthesized, unnatural nucleotide. The engineered homeodomain preferentially binds to the modified DNA with affinity and specificity similar to those of natural homeodomains. Copyright

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CO2 capture with alkanolamines has been in use since 1930, where 2-ethanolamine (MEA) is the most studied absorbent for post-combustion. In order to prevent degradation, it is important to understand the degradation mechanisms, which in turn requires knowledge of both stoichiometry and kinetics of the reactions and chemical pathways associated with degradation. In the present work thermal degradation with CO2 in closed cylinders at 135C is performed on already oxidatively degraded solutions from both an open batch and a closed batch setup. Thermal degradation with CO2 on oxidatively degraded solutions seems to give typical thermal degradation compounds.

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Oxazolidin-2-ones and imidazolidin-2-ones are prepared under mild reaction conditions by DMAP-catalyzed isocyanation of 1,2-aminoalcohols and 1,2-diamines with di-tert-butyl dicarbonate and subsequent cyclization.

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The present invention relates generally to substituted isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds

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2-oxazolones were synthesized from 2-oxazolidinones utilizing anodic oxidation as the key step.

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A stereocontrolled total synthesis of (+)-vinblastine was accomplished, featuring preparations of the two indole units by means of a novel indole synthesis via radical cyclization of thioanilide, and a stereoselective coupling of these units. Copyright

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The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently C(H)= or N=, provided that at least one of A and B is -N=, n is 1-3, m is 0-3, and R14 are as defined herein.

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The synthesis of racemic Carvedilol ((±)-1) has been achieved starting from 2-(chloromethyl) oxirane ((±)-2) in a four-step sequence. 5-(Chloromethyl) oxazolidin-2-one ((±)-3) and 5-((9Hcarbazol-4-yloxy) methyl) oxazolidin-2-one ((±)-4) are intermediates. A similar sequence starting from (R)- or (S)-2-(chloromethyl)oxirane 2 give corresponding chiral 5-((9Hcarbazol-4-yloxy)methyl) oxazolidin-2-one 4 followed by chiral Carvedilol 1. The synthetic sequence followed avoids the formation of impurity B (bis impurity). This approach can be useful for the preparation of pharmaceutically important moieties containingbeta-amino alcohols without formation of bis impurity.

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The scope of the three-component reaction of aldehydes, amides, and dienophiles, the so-called AAD reaction, is extended to the formation of 2- and 3-bromo-substituted 1-amido-2-cyclohexene derivatives. The incorporation of the halogen substituent allows further elaboration of this interesting class of products. Georg Thieme Verlag Stuttgart.

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Arylation of a diverse group of N-H containing compounds at room temperature with triarylbismuth and cupric acetate in the presence of a tertiary amine promoter, such as triethylamine or pyridine, is described. This mild and highly efficient procedure, which is based on Barton’s earlier work on the arylation of amines, can be applied to amides, imides, ureas, carbamates, and sulfonamides. Copyright (C) 1996 Elsevier Science Ltd.

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