Synthesis and [11C]-radiolabelling of dechloro-epibatidine and 2PABH, two potential radioligands for studying the central nAChRs in vivo
The two epibatidine (EPB) analogues dechloro-epibatidine (DCl-EPB) and 2PABH were synthesised via a two step reaction starting from N-methoxycarbonyl-7-azabicyclo[2.2.1]heptene. The radiochemical syntheses of [11C]N-methylated derivatives was performed using the classical methylating agent [11C]CH3I in acetonitrile. The radiochemical yield ranged from 5 to 10% (decay corrected from [11C]CH3I) and was fully sufficient for small animal experiments. High specific activities in the range of 140 to 360 GBq/μmol at EOS (end of synthesis) were obtained. The radiosynthesis, semipreparative HPLC, formulation and quality control were completed in an average time of 35 min.
Spang,Patt,Westera,Schubiger
p. 761 - 771
(2007/10/03)
Stereocontrolled Total Synthesis of (+)- and (-)-Epibatidine
The stereocontrolled total synthesis of the novel analgesic agent (-)-epibatidine (1) and its enantiomer starting with 6-chloropyridine-3-carboxaldehyxe (2) has been carried out by way of intermediates 3-10.
Corey, E. J.,Loh, Teck-Peng,AchyuthaRao, Sidduri,Daley, Donnette C.,Sarshar, Sepehr
p. 5600 - 5602
(2007/10/02)
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