摘要
5-碘-2,3-二甲氧基苯甲酸与(S)-1-烯丙基-2-氨甲基吡咯烷反应得到(S)-(–)-N-[(1-烯丙基-2-吡咯烷基)甲基]-2,3-二甲氧基-5-碘苯甲酰胺,与双三丁基锡反应得到标记前体(S)-(–)-N-[(1-烯丙基-2-吡咯烷基)甲基]-2,3-二甲氧基-5-三丁基锡苯甲酰胺,总收率约70%。用双氧水法对标记前体进行碘[131I]标记得到SPECT显像剂131I-nalepride,标记率和放射化学纯度分别为95.4%和96.3%。
131↑I-Nalepride, a SPECT imaging agent was synthesized from the precursor, (S)-N-((1- allylpyrrolidin-2-yl) methyl]-2,3-dimethoxy-5-tributylstannanylbenzaminde by using Na131↑I and oxidation in situ with hydrogen peroxide in 95.4% radiolabelled yield and 96.3% radiochemical purity. The precursor was synthesized from 2,3-dimethoxy-5-iodobenzoic acid via amidation with (S)- 1-allyl-2-aminomethylpyrrolidine to give the key intermediate (S) -N- E (1-allylpyrrolidin-2-yl) methyl]-2,3-dimethoxy-5-iodobenzamide, followed by reaction with (C4H9) 6Sn2 with an overall yield of about 70%.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2008年第3期166-168,共3页
Chinese Journal of Pharmaceuticals
基金
国家自然基金(30670714)
江苏省高技术研究计划(BG2006604)
江苏省卫生厅项目(H200334)
江苏省医学重点人才资助(RC2007096)