Synthesis of novel hapten derivatives of 1alpha,25-dihydroxy-vitamin D3 and its 20-epi analogue |
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Authors: | Blaehr Lars K A Björkling Fredrik Calverley Martin J Binderup Ernst Begtrup Mikael |
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Institution: | Medicinal Chemistry Research, LEO Pharma, DK-2750 Ballerup, Denmark. lars.blaehr@leo-pharma.com |
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Abstract: | Hapten derivatives of 1alpha,25-dihydroxyvitamin D(3) and its 20-epimer were synthesized and conjugated to a carrier protein for raising polyclonal antibodies. The haptens were linked through spacers at C-16, thereby exposing both the A-ring and the side chain of the molecules, to maximize antibody specificity. The spacers were introduced via stereoselective hydroboration of 16-ene intermediates as the key step. In immunoassays, the antibodies raised toward the natural hormone were selective to this compound over derivatives with modifications in the A-ring or the side chain. The antibodies toward the 20-epimer, however, were unable to recognize modifications in the side chain. |
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