32046-43-8Relevant articles and documents
DERIVATIVES OF 6,7-DIHYDRO-5H-IMIDAZO[1,2-α]IMIDAZOLE-3- CARBOXYLIC ACID AMIDES
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Page/Page column 112-113, (2009/07/03)
Derivatives of 6,7-dihydro-5H-imidazo[1,2-α]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.
Comparison of two synthetic methods to obtain [18F] N-(2-aminoethyl)-5-fluoropyridine-2-carboxamide, a potential MAO-B imaging tracer for PET
Beer,Haerberli,Ametamey,Schubiger
, p. 933 - 945 (2007/10/02)
The compound Ro 19-6327, N-(2-aminoethyl)-5-chloropyridine-2-carboxamide, is known to inhibit reversibly and site specifically the enzyme monoamine oxidase B (MAO-B). The 123I-labelled iodo-analogue N-(2-aminoethyl)-5-iodopyridine-2-carboxamide (Ro 43-0463) was investigated successfully in human volunteers by means of SPET (Single Photon Emission Tomography). We developed therefore the synthesis and radiolabelling of the corresponding fluoro-analogue N-(2-aminoethyl)-5-fluoropyridine-2-carboxamide with 18F in order to carry out PET (Position Emission Tomography) investigations of MAO-B related neuropsychiatric diseases. For this purpose two synthetic approaches leading to the electrophilic and the nucleophilic methods of 18F radiolabelling were undertaken. The nucleophilic approach appeared to be superior when factors such as precursor synthesis, beam time, specific activity and radiochemical purity of the product are considered.
The preparation of Some 4- and 5-Substituted Pyridine-2-carboxylic Acids as Fusaric Acid Analogues.
Oehlke, J.,Schroetter, E.,Dove, S.,Schick, H.,Niedrich, H.
, p. 591 - 596 (2007/10/02)
In view of future studies on the structure-activity relationships involved in the inhibition of dopamine β-hydroxylase, the authors synthetized 5-substituted picolinic acids and 4-substituted fusaric acids selected by means of a random sampling procedure suited for small series.On this occasion, they succeeded in improving markedly the well-known synthesis of 5-nitropicolinic acid via a Rosenmund-v.Braun reaction with 2-bromo-5-nitropyridine. 5-Hydroxypicolinic acid which is easily accessible in the same way could be converted into 5-alkyloxypicolinic acids by reaction with alkyl halides in DMSO in the presence of silver oxide. 4-Substituted fusaric acids became accessible via 5-n-butyl-2-methyl-4-nitropyridine-N-oxide.