| 摘要 |
Disclosed is a method for preparing vitamin B12 (VB12) derivatives suitable for linking to a polymer, nanoparticle or therapeutic agent, protein or peptide comprising the steps of reacting the 5' OH group of VB12 or an analogue thereof with a bifunctional carbonyl electrophile to form an active intermediate, and subsequently reacting the intermediate with a nucleophilie spacer molecule to yield said VB12 derivative, wherein the bifunctional carbonyl electrophile is selected from the group consisting of carbonyldiimidazole phosgene, triphosgene, N,N disuccinimidyl carbonate, carbonyl dipiperidine, 1,1'-carbonyldi(1,2,4-triazole), di(2-pyridyi)ketone or di(1- benzotriazolyl)carbonate. Also disclosed are specific 5' OH modified derivatives of VB12.
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