- Water-soluble adamantane-terminated dendrimers possessing a rhenium core
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A novel type of radiometal-containing dendrimer with potential radiotherapeutical applications is described. Different generations of this adamantane-terminated, Frechet-type dendrimer (28, 29, 30), each consisting of two dendritic wedge ligands around a rhenium core, have been synthesized in organic solvent via reaction with ReO(PPh3)2Cl3. Through complexation of their adamantane groups by β-cyclodextrins (β-CDs), these dendrimers were made water soluble (9.6, 0.4, and 0.2 mM, respectively). β-CD-induced solubilization of the wedges in water allowed the complexes to be made under aqueous conditions, via reaction with rhenium gluconate. Not only does this strategy enable the facile synthesis of the radioactive analogue, the yields for these complex-formation reactions in water also turned out to be far higher than those observed for the reactions in organic solvents.
- Van Bommel,Metselaar,Verboom,Reinhoudt
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- Chemical Transformations of Tetracyclo[3.3.1.13,7.01,3]decane (1,3-Dehydroadamantane): VII. Reaction of 1,3-Dehydroadamantane with Alkanediols and Amino Alcohols
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The reaction of 1,3-dehydroadamantane with C2–C6 α,ω-alkanediols selectively afforded ω-(adamantan- 1-yloxy)alkan-1-ols in 87–94% yield. The reaction of 1,3-dehydroadamantane with ω-aminoalkan-1- ols (2-aminoethanol and 3-aminopropan-1-ol) gave mixtures of addition products through the oxygen and nitrogen atoms, which can be readily separated by fractional vacuum distillation or crystallization.
- Butov,Mokhov
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p. 1760 - 1763
(2019/03/26)
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- ORGANIC COMPOUNDS
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The application relates to novel substituted piperidines of the general formula (I) in which R1, R2, R3, R4, W, X, Z, m and n are each as defined in detail in the description, to a process for their preparation and to the use of these compounds as medicines, in particular as renin inhibitors.
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Page/Page column 46
(2010/02/15)
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