Chinese Journal of Applied Chemistry

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Synthesis and Characterization of Phenylmethanesulfonamide Ligand for Potential Labeling [99mTc(CO)3(H2O)3]+

CHEN Yongshi1,2, LIN Jianguo2*, QIU Ling2, CHENG Wen2, LUO Shineng2, MA Haixia1*   

  1. (1.School of Chemical Engineering,Northwest University,Xi′an 710069,China;
    2.Key Laboratory of Nuclear Medicine of Ministry of Healthy,Jiangsu Key Laboratory of
    Molecular Nuclear Medicine,Jiangsu Institute of Nuclear Medicine,Wuxi 214063)
  • Received:2011-07-25 Revised:2011-10-20 Published:2012-07-10 Online:2012-07-10

Abstract: A new ligand N-[2-cyclohexylmethoxy-4(1-(2,2′-bipyridinemethyl)amino)acetylamino] phenylmethanesulfonamide(NSC-PA), for potential labeling [99mTc(CO)3(H2O)3]+ was synthesized by hydroxyl-alkylation, amino-methylsulfonylation, nitro-reduction, amino-bromideacetylation and N-alkylation from 2-amino-5-nitrophenol. Simple experimental operation, short period and purified products could be obtained under optimized conditions. The structures of all the compounds were confirmed by 1H NMR, IR and MS. The purity of the target compound was over 98% as given by HPLC result. The target product could be used for future labeling studies. This synthesis is promising in the exploration of new imaging reagent for breast cancer.

Key words: phenylmethanesulfonamide, synthesis, optimization, labeling ligand

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