【药物名称】(R)-FIPCT
化学结构式(Chemical Structure):
参考文献No.567344
标题:Synthesis, biodistribution, and primate imaging of fluorine-18 labeled 2 beta-carbo-1'-fluoro-2-propoxy-3beta-(4-chlorophenyl)tropanes. Ligands for the imaging of dopamine transporters by positron emission tomography
作者:Xing, D.; Chen, P.; Keil, R.; Kilts, C.D.; Shi, B.; Camp, V.M.; Malveaux, G.; Ely, T.; Owens, M.J.; Votaw, J.; Davis, M.; Hoffman, J.M.; BaKay, R.A.; Subramanian, T.; Watts, R.L.; Goodman, M.M.
来源:J Med Chem 2000,43(4),639
合成路线图解说明:

Treatment of (S)-glycidol (I) with triphenylmethyl chloride (Ph3CCl) in pyridine affords O-triphenylmethylglicydyl ether (II), which is then reduced with LiAlH4 in THF to provide alcohol (III). Hydrogenolysis of (III) over Pd/C in MeOH gives 1,2-propandiol (IV), which is then mesylated by means of methanesulfonyl chloride (MsCl) and Et3N in CH2Cl2 to furnish 1-mesyloxy-2-propanol (V). Treatment of tropane (VI) with a refluxing mixture of dioxane/H2O yields carboxylic acid (VII), which is converted into acid chloride (VIII) by means of phosphorus oxychloride (POCl3). Coupling of alcohol (V) with acid chloride (VIII) and Et3N in CH2Cl2 gives tropane derivative (IX), which is finally converted into the target compound by fluorination with tetrabutylammonium fluoride (TBAF) in THF.

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