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J Org Chem ; 73(21): 8236-43, 2008 Nov 07.
Artigo em Inglês | MEDLINE | ID: mdl-18826327

RESUMO

A convenient method for the preparation of fluorous aryl stannanes was developed as a means of expanding the general utility of the fluorous labeling strategy (FLS). Following the synthesis of a novel fluorous distannane, a palladium-catalyzed cross-coupling reaction was used to prepare the target compounds from aryl halides. The scope of the reaction was investigated by preparing a small library of model compounds where the reaction yields were similar to those reported for the analogous procedures employing hexamethyl- or hexabutyldistannanes. The utility of the reported methodology was demonstrated through the successful synthesis of fluorous precursors to two established molecular imaging and therapy agents (FIAU, IUdR). These were radiolabeled with iodine-125 and the desired products isolated in high yield and effective specific activity.


Assuntos
Marcação por Isótopo/métodos , Compostos de Estanho/química , Estanho/química , Catálise , Reagentes de Ligações Cruzadas , Radioisótopos do Iodo , Métodos , Paládio
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