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Solid-Phase Preparation (solid-phase + preparation)

Distribution by Scientific Domains
Chemistry100%

Selected Abstracts

Solid-Phase Preparation of a Library Based on a Phenylalanine Scaffold

MOLECULAR INFORMATICS, Issue 8 2005
Aina Colombo
Abstract A convenient strategy (preliminary study, preproduction and production) for the solid-phase preparation of a library using 4-iodophenylalanine as a scaffold is described. The aromatic ring was first modified via the Suzuki reaction and the amino position was subsequently derivatized into amides, sulfonamides, amines, carbamates and ureas. The scope and limitations of all of the reactions carried out in parallel are discussed. The solid-phase synthesis of a library of 315 individual compounds was attempted by using seven boronic acids and nine representative compounds from each of the following classes: carboxylic acids, sulfonyl chlorides, aldehydes, alcohols and isocyanates. Owing to the failure of the amine derivatization, 297 compounds were ultimately obtained. [source]

Improved Solution- and Solid-Phase Preparation of Hydroxamic Acids from Esters.

CHEMINFORM, Issue 43 2005
Chih Y. Ho
Abstract For Abstract see ChemInform Abstract in Full Text. [source]

Solid-Phase Preparation of a Library Based on a Phenylalanine Scaffold

MOLECULAR INFORMATICS, Issue 8 2005
Aina Colombo
Abstract A convenient strategy (preliminary study, preproduction and production) for the solid-phase preparation of a library using 4-iodophenylalanine as a scaffold is described. The aromatic ring was first modified via the Suzuki reaction and the amino position was subsequently derivatized into amides, sulfonamides, amines, carbamates and ureas. The scope and limitations of all of the reactions carried out in parallel are discussed. The solid-phase synthesis of a library of 315 individual compounds was attempted by using seven boronic acids and nine representative compounds from each of the following classes: carboxylic acids, sulfonyl chlorides, aldehydes, alcohols and isocyanates. Owing to the failure of the amine derivatization, 297 compounds were ultimately obtained. [source]

Preparation of Tripeptide-Bridged Dicatechol Ligands and Their Macrocyclic Molybdenum(VI) Complexes: Fixation of the RGD Sequence and the WKY Sequence of Urotensin II in a Cyclic Conformation

CHEMISTRY - A EUROPEAN JOURNAL, Issue 15 2004
Markus Albrecht Prof. Dr.
Abstract Dicatechol ligands were prepared with caprylic acid (6 -H4) or the naturally occurring RGD (23 -H4) or WKY sequences (32 -H4) as spacers. 6 -H4 was prepared by solution-phase amide coupling chemistry, while 16, the precursor of 23 -H4, was obtained by solution-phase and solid-phase preparation. In the latter case, a polystyrene resin with a hydrazine benzoate linker was used as the solid support. The last coupling step was performed simultaneously with cleavage of the peptide from the resin. The protecting groups of 16 were all removed in one step to yield the free ligand 23 -H4. The WKY-bridged derivative 32 -H4 was obtained by a similar solid-phase synthesis followed by deprotection. The reaction of all three ligands with dioxomolybdenum(VI) bis(acetylacetonate) afforded 19-membered metallamacrocycles in which the short peptides are conformationally fixed in a turn-type structure. Hereby, the side-chain functionalities of the peptides do not interfere in the metal complexation. [source]