- New [11C]phosgene based synthesis of [11C]pyrimidines for positron emission tomography
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Thymine, 5-FU, and uracil were successfully synthesized through a procedure involving a cyclocondensation of triphosgene with newly developed (α-substituted β-aminoacrylamides intermediates (1a, X= Me; 1b, X= F; 1c, X= H). The radioligands [2-11C]thymine and [2- 11C]5-fluorouracil were synthesized in high radiochemical yields in 16-17 minutes from the end of bombardment by applying the cyclocondensation method with [11C]COCl2.
- Seki, Koh-Ichi,Nishijima, Ken-Ichi,Sanoki, Kimihito,Kuge, Yuji,Takahashi, Masayuki,Akizawa, Hiromichi,Tamaki, Nagara,Wiebe, Leonard I.,Ohkura, Kazue
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experimental part
p. 1307 - 1321
(2010/10/03)
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- Nucleic acid derivatives
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A compound which comprises a backbone having a plurality of chiral carbon atoms, the backbone bearing a plurality of ligands each being individually bound to a chiral carbon atom of the plurality of chiral carbon atoms, the ligands including one or more pair(s) of adjacent ligands each containing a moiety selected from the group consisting of a naturally occurring nucleobase and a nucleobase binding group, wherein moieties of the one or more pair(s) are directly linked to one another via a linker chain; building blocks for synthesizing the compound; and rises of the compound, particularly in antisense therapy.
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- THE BENZOYLATION OF URACIL AND THYMINE
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Uracil and thymine react with benzoyl chloride in acetonitrile-pyridine solution at room temperature to give first their 1-N-benzoyl (2b and 3b) and then their 1-N,3-N-dibenzoyl derivatives (4a and 4b, respectively); the latter compounds are converted into the corresponding 3-N-benzoyl derivatives (5a and 6a) under mild conditions of basic hydrolysis.
- Cruickshank, Kenneth A.,Jiricny, Josef,Reese, Colin B.
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p. 681 - 684
(2007/10/02)
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