【药物名称】CPFPX
化学结构式(Chemical Structure):
参考文献No.478246
标题:A1 adenosine receptor antagonists as ligands for positron emission tomography (PET) and single-photon emission tomography (SPET)
作者:Holschbach, M.H.; Fein, T.; Krummeich, C.; Lewis, R.G.; Wutz, W.; Schwabe, U.; Unterlugauer, D.; Olsson, R.A.
来源:J Med Chem 1998,41(4),555
合成路线图解说明:

The cyclization of N-benzyl-N'-propylurea (I) with cyanacetic acid (II) in hot acetic anhydride gives 6-amino-1-benzyl-3-propyluracil (III), which is nitrosated with NaNO2/acetic acid and reduced with sodium dithionite to yield 5,6-diamino-1-benzyl-3-propyluracil (IV). The cyclization of (IV) with cyclopentylcarbonyl chloride (V) by means of NaOH in refluxing ethanol affords 3-benzyl-8-cyclopentyl-1-propylxanthine (VI), which is acylated with pivaloyl chloride (VII)/Na2CO3 in DMF giving the expected 7-acyl derivative (VIII). The debenzylation of (VIII) by hydrogenation over Pd/C as usual yields 8-cyclopentyl-7-pivaloyl-1-propylxanthine (IX), which is condensed with 1-bromo-3-fluoropropane (X) by means of Na2CO3 in DMF to afford 8-cyclopentyl-3-(3-fluoropropyl)-7-pivaloyl-1-propylxanthine (XI). Finally, this compound is deprotected with NaOH in DMSO/water.

参考文献No.700045
标题:Synthesis and evaluation of no-carrier-added 8-cyclopentyl-3-(3-[(18)F]fluoropropyl)-1-propylxanthine ([(18)F]CPFPX): A potent and selective A1-adenosine receptor antagonist for in vivo imaging
作者:Holschbach, M.H.; Olsson, R.A.; Bier, D.; Wutz, W.; Sihver, W.; Sch黮ler, M.; Palm, B.; Coenen, H.H.
来源:J Med Chem 2002,45(23),5150
合成路线图解说明:

The reaction of 8-cyclopentyl-3-(3-hydroxypropyl)-1-propylxanthine (I) with Ts-Cl and TEA gives the corresponding tosylate (II), which is then radiolabeled by means of 18FK and Kryptofix to provide the target radiolabeled compound.

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