50373-10-9Relevant articles and documents
METHOD FOR THE PREPARATION OF N-MONOFLUOROALKYL TROPANES AND THEIR USE
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Page/Page column 15, (2021/07/31)
The present invention relates to a method for the preparation of an N-monofluoroalkyl tropane, a method for the preparation of a trialkyltin tropane, a method for the preparation of an iodinated and/or radioiodinated tropane and the use of the N-monofluoroalkyl tropane as a precursor in the method for the preparation of the trialkyltin tropane and/or the iodinated and/or radioiodinated tropane.
Synthesis of 3-arylecgonine analogues as inhibitors of cocaine binding and dopamine uptake
Kline Jr.,Wright,Fox,Eldefrawi
, p. 2024 - 2027 (2007/10/02)
3-Arylecgonine analogues were synthesized and characterized by 1H and 13C NMR, IR, and MS. The compounds were synthesized as racemates from cycloheptatriene-7-carboxylic acid or enantiomerically from (-)-cocaine. These analogues were tested for their ability to inhibit [3H]cocaine binding to bovine striatal tissue and to inhibit [3H]dopamine uptake into striatal synaptosomes. Methyl (1RS-2-exo-3-exo)-8-methyl-3-phenyl-8-azabicyclo[3.2.1]octane-2-carboxylate was the most potent analogue. IC50 values for inhibition of cocaine binding and dopamine uptake were 20 and 100 nM, respectively. The racemates and the 1R isomers were equally potent inhibitors of binding and uptake. Methyl (1RS-2-endo-3-exo)-3-(2,4-dinitrophenyl)-8-methyl-8- azabicyclo[3.2.1]octane-2-carboxylate was the least potent. IC50 for inhibition of both binding and uptake was 40 μM.