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2.
J Comb Chem ; 3(3): 312-8, 2001.
Artigo em Inglês | MEDLINE | ID: mdl-11350255

RESUMO

The synthesis and use of an alkylsilyl-tethered large (500-600 microm) polystyrene resin (1) are disclosed. An optimized Suzuki coupling of bromine-functionalized polystyrene and a silicon-functionalized alkylborane generates the silicon-substituted polystyrene 1 in large scale (>100 g). Resin loading is accomplished by activation as the silyl triflate, which can accommodate even sterically encumbered secondary alcohols and phenols. Treatment with HF/pyridine for linker cleavage is mild, efficient, and amenable to an automated, large-scale distribution system. This platform delivers, minimally, 50 nmol of each small molecule derived from a diversity-oriented, split-pool synthesis on a per bead basis for use in both forward and reverse chemical genetic assays. This technology satisfies many requirements of a one bead-one stock solution approach to chemical genetics.


Assuntos
Sistemas de Liberação de Medicamentos , Poliestirenos/síntese química , Alcinos/química , Bromo/química , Sistemas de Liberação de Medicamentos/instrumentação , Sistemas de Liberação de Medicamentos/métodos , Desenho de Fármacos , Microesferas , Estrutura Molecular , Poliestirenos/química , Resinas Vegetais/química , Silanos/química , Relação Estrutura-Atividade
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