- Crown Ether Nucleophilic Catalysts (CENCs): Agents for Enhanced Silicon Radiofluorination
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New bifunctional phase transfer agents were synthesized and investigated for their abilities to promote rapid fluorination at silicon. These agents, dubbed crown ether nucleophilic catalysts (CENCs), are 18-crown-6 derivatives containing a side-arm and a potentially nucleophilic hydroxyl group. These CENCs proved efficacious in the fluorination of hindered silicon substrates, with fluorination yields dependent on the length of linker connecting the metal chelating unit to the hydroxyl group. The efficacy of these CENCs was also demonstrated for rapid radiofluorination under mild conditions for eventual application in molecular imaging with positron emission tomography (PET). The hydrolysis-resistant aryl silicon fragment is promising as a convenient synthon for labeling potential PET radiotracers.
- Jana, Susovan,Al-Huniti, Mohammed H.,Yang, Bo Yeun,Lu, Shuiyu,Pike, Victor W.,Lepore, Salvatore D.
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p. 2329 - 2335
(2017/03/11)
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- Folding of alternating dialkylsilylene-spaced donor-acceptor copolymers: The oligomer approach
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A series of oligmers with donor-acceptor pairs separated by diisopropylsilylene (iPr2Si) spacers, composed of monomer 4b, dimer 5, trimer 6, and tetramer 7, were synthesized to scrutinize the folding behavior. Monomer 4a with a dimethylsilylene (Me2Si) spacer was also prepared for comparison. The 4-aminostyrene moiety was used as the donor and the stilbene moiety as the acceptor. Both steady-state and time-resolved fluorescence spectroscopic measurement were made. Regardless of the substituents on the silicon atom, the emission spectra of 4a and 4b exhibit both local excited (LE) emission of the acceptor chromophore and emission from the charge-separated state (CT emission), which are similar to that of the corresponding Me2Si-spaced copolymer 2a with the same donor and acceptor chromophores, but different from that of the copolymer with the iPr2Si spacer 2b. Dimer 5 behaves like 4 and 2a. As the chain length of the oligomers increases, the emission properties of the higher homologues become prone to that of 2b. Thus, tetramer 7 exhibits emission from the charge-transfer complex, which is essentially same as that of 2b. Moreover, charge-transfer absorptions emerge in 6 and 7. These results suggest that the folding nature of oligomers approaches that of the corresponding polymer, as the degree of oligomerization increases, and the electronic interactions between adjacent donor-acceptor pairs are controlled by the steric effect of the substituents on the silicon atoms and concomitant amplification of the stabilizing energy by extending the distance of the folding structure. Copyright
- Chen, Chih-Hsien,Chen, Wen-Hao,Liu, Yi-Hung,Lim, Tsong-Shin,Luh, Tien-Yau
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scheme or table
p. 347 - 354
(2012/03/09)
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- Introduction of 3-terminal nucleosides having a silyl-type linker into polymer supports without base protection
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New 3 -terminal deoxyribonucleoside-loading reagents having a silyl-type linker were developed. They were effectively introduced into polymer supports under the conditions of Huisgen [3 + 2] cycloaddition without base protection. Moreover, four unmodified
- Ohkubo, Akihiro,Noma, Yasuhiro,Aoki, Katsufumi,Tsunoda, Hirosuke,Seio, Kohji,Sekine, Mitsuo
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experimental part
p. 2817 - 2823
(2009/08/08)
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- Silicon-derivates for PET-Imaging
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This invention relates to silicon-derivated compounds suitable for labelling or already labelled with 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging, preferably positron emission tomography (PET).
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Page/Page column 18
(2008/06/13)
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- Silicon derivatives for PET imaging
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This invention relates to silicon-derivated compounds suitable for labelling or already labelled with 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of
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Page/Page column 15-16
(2010/11/30)
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- 3'-TERMINAL NUCLEOSIDE UNIT CONTAINING PHOSPHORAMIDITE
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The purpose of the present invention is therefore to provide a method for binding a 3'-end nucleoside unit comprising any base to a hydroxyl group on a solid-phase support under completely the same condition as in DNA chain elongation reaction. The presen
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- Dioxanes and uses thereof
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In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (I) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p. The present invention also provides methods for preparing compounds of the invention.
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- Dioxanes and uses thereof
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In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel compounds of general formula (I): and pharmaceutically acceptable derivatives thereof, wherein R1, R2, R3, n, X and Y are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I) and a pharmaceutically acceptable carrier. The present invention further provides compounds capable of inhibiting histone deacetylatase activity and methods for treating disorders regulated by histone deacetylase activity (e.g., cancer and protozoal infections) comprising administering a therapeutically effective amount of a compound of formula (1) to a subject in need thereof. The present invention additionally provides methods for modulating the glucose-sensitive subset of genes downstream of Ure2p.
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- Synthesis of 7200 small molecules based on a substructural analysis of the histone deacetylase inhibitors trichostatin and trapoxin.
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Seventy-two hundred potential inhibitors of the histone deacetylase (HDAC) enzyme family, based on a 1,3-dioxane diversity structure, were synthesized on polystyrene macrobeads. The compounds were arrayed for biological assays in a "one bead-one stock sol
- Sternson,Wong,Grozinger,Schreiber
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p. 4239 - 4242
(2007/10/03)
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