- THIAZOLE DERIVATIVES AS ALPHA 7 NACHR MODULATORS
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Disclosed is a compound of formula (I) wherein Y, Ring D, m and R1-R4 are as described herein, as a modulator of nicotinic acetylcholine receptors particularly the α7 subtype, in a subject in need thereof, as well as pharmaceutically acceptable salts, polymorphs, solvates, and isomers thereofs, for use either alone or in combinations with suitable other medicaments, and pharmaceutical compositions containing such compounds. Also disclosed are a process of preparation of the compounds and the intended uses thereof in therapy, particularly in the prophylaxis and therapy of disorders such as Alzheimer's disease, mild cognitive impairment, senile dementia, and the like.
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Page/Page column 58
(2013/09/26)
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- PREPARATION OF FLUORINE-LABELLED COMPOUNDS
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The invention relates to a process for producing a fluorine-labelled compound, the process comprising: (a) treating a compound of formula (I) wherein R1, R2 and the C(H) group to which R1 and R2 are bonded together form a moiety to be labelled with fluorine; and the fluorous tag is a group of formula (II) wherein Rf is a straight-chained or branched C4-I2 perfluoroalkyl group; and L is a single bond, -alk-, -arylene-, -alk-arylene-, alk-X-, -arylene-X-, -alk-arylene-X, -alk- X-arylene-, -alk-X-arylene-X-, -arylene-alk-, -arylene-X-alk-, -arylene-alk-X- or - arylene-X-alk-X-, wherein X is N(R ), O, S, C(O) or C(O)N(R ) and wherein alk is unsubstituted or substituted C1-10 alkylene which is optionally interrupted by N(R ), O, S, C(O), C(O)N(R ) or arylene, wherein R is C1-6 alkyl or aryl; with [nF], wherein nF is 18F or 19F, thereby fluorinating and detagging the compound of formula (I) to produce a fluorine-labelled compound of formula (III) The invention further relates to compounds of formula (I), a process for producing such compounds, and a combination product which comprises the two reactants used in that process.
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Page/Page column 82
(2010/04/03)
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- Fluorous synthesis of 18F radiotracers with the [ 18F]fluoride ion: Nucleophilic fluorination as the detagging process
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Tag team: The flouro-detagging of flourous sulfonates by the [ 18F]fluoride ion was found to be an advantageous strategy for the preparation of various 18F-labeled prosthetic groups and known radiotracers (see picture). Fluorous solid phase extraction (FSPE) was used to separate the excess fluorous precursor from the labeled material, which suggests that traditional purification protocols such as distillation or tedious separation can be avoided. (Chemical Equation Presented).
- Bejot, Romain,Fowler, Thomas,Carroll, Laurence,Boldon, Sophie,Moore, Jane E.,Declerck, Jerome,Gouverneur, Veronique
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supporting information; experimental part
p. 586 - 589
(2009/04/14)
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