- Synthesis and ex vivo evaluation of carbon-11 labelled N-(4-methoxybenzyl)- N′-(5-nitro-1,3-thiazol-2-yl)urea ([11C]AR-A014418): A radiolabelled glycogen synthase kinase-3β specific inhibitor for PET studies
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N-(4-Methoxybenzyl)-N′-(5-nitro-1,3-thiazol-2-yl)urea (AR-A014418), a highly selective inhibitor of glycogen synthase kinase-3β (GSK-3β), was radiolabelled with carbon-11 (half-life = 20.4 min) for cerebral positron emission tomography (PET) studies. Reac
- Vasdev, Neil,Garcia, Armando,Stableford, Winston T.,Young, Alex B.,Meyer, Jeffrey H.,Houle, Sylvain,Wilson, Alan A.
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p. 5270 - 5273
(2007/10/03)
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- Diastereotopic Group Selective Intramolecular Conjugate Addition of 4-(2-Hydroxyethyl)-p-Quinol Derivatives: Synthesis of the Optically Pure cis-7-Oxabicyclonon-2-en-4-one Skeleton.
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Diastereotopic group selective cyclization of 4-(2-hydroxyethyl)-p-quinol derivatives was achieved and the reaction applied to the synthesis of the optically pure cis-7-oxabicyclonon-2-en-4-one skeleton.
- Fujioka, Hiromichi,Kitagaki, Shinji,Ohno, Naoko,Kitagawa, Hidetoshi,Kita, Yasuyuki,Matsumoto, Keita
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p. 333 - 336
(2007/10/02)
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- Syntheses and Reactions of (Trimethylsiloxy)benzoyl Chlorides
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The (trimethylsiloxy)benzoyl chlorides 1-7 are easily to obtain under mild conditions from silylated hydroxybenzoic acids by means of thionyl chloride.Whereas these acid chlorides are stable at room temperature, they undergo condensation polymerisation at temperatures above 100 deg C.Reactions with various nucleophils, such as thioalcohols, phenols, amines, N,O-bis(silylated)amino acids and N-silylated lactams were investigated.With hexamethyldisilazane and thionyl chloride the (trimethylsiloxy)benzonitriles 21, 22 are accessible, and by means of trimethylsilylazide the (trimethylsiloxy)phenyl isocyanates 23-25 were obtained.Conversion with phenyl carbazate and subsequent silylation lead to the 2-(trimethylsiloxy)phenyl-1,3,4-oxadiazol-5-ones 27a-c.
- Schwarz, Gerd,Alberts, Heinrich,Kricheldorf, Hans R.
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p. 1257 - 1270
(2007/10/02)
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