Adamczyk M, Chen Y Y, Moore J A, Mattingly P G
Department of Chemistry, Abbott Laboratories, Abbott Park, IL 60064-3500, USA.
Bioorg Med Chem Lett. 1998 Jun 2;8(11):1281-4. doi: 10.1016/s0960-894x(98)00225-x.
3-O-tert-Butyldimethylsilyl-17 alpha-(6-mesyloxyhexynyl)estradiol was converted to the azide in 60-70% yield with NaN3/DMPU, then reduced to the corresponding amine (> 95% yield). Acylation with the N-hydroxysuccinimide esters of biotin, 5-carboxyfluorescein and 10-(3-sulfopropyl)-N-tosyl-N-(3- carboxypropyl)acridinium-9-carboxamide gave the title conjugates. The KDs of the tracers with an estradiol antibody ranged from 97-197 nM.
