Phosphonate-free phosphorylation of alcohols using bis-(tert-butyl) phosphoramidite with imidazole·hydrochloride and imidazole as the activator |
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Authors: | Bruno Haché Lisa BrettSagar Shakya |
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Institution: | Array BioPharma Inc., 2620 Trade Centre Ave, Longmont, CO 80503, USA |
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Abstract: | A variety of commercially available alcohols were converted to their bis-(tert-butyl) protected mono-phosphate pro-drugs. The improved procedure uses the unique combination of imidazole·hydrochloride and imidazole as the activator to suppress the formation of undesired phosphonate by-product frequently encountered with the bis-(tert-butyl) phosphoramidite reagents. The new activation procedure eliminates the need to use excess reagents. |
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