一种亲肿瘤二肤的合成研究.PDF

CNIC-01991 CAEP-0254 一种亲肿瘤二肤的合成研究 何佳恒 (中国工程物理研究院核物理与化学研究所，绵阳，621900) 摘要 针对日益升高的肿瘤发病率，开发放射性药物具有十分积极的 意义，而合成放射性药物前体是制备放射性药物的必要前提D 为了 寻求一种能抑制绝大多数(85% 以上)癌细胞中含有的端粒体酶，从 而得到治疗肿瘤的化合物，设计了一种新的放射性药物前体一一一叔 丁氧毅基二肤胶磷耽对哄苯盼酶，合成了该化合物及其稳定的中间 体O 目标产品经元素分析、核磁共振、质谱等表征，结果表明，配体的 合成是成功的o 在合成过程中，采用液相法代替了传统的回相合成 法，降低了合成成本，提高了可操作性o 关键词:放射性药物前体苯盼液相法 202 The Synthesis of a Kind of Dipeptide (1η Chinese) HE Jiaheng CInstitute of Nuclear Physics and Chemistry , CAEP , Mianyang , 621900) ABSTRACT The research on novel radioiodopharmaceutical which treat tumor efficient- ly is meaningful , moreover , this result just base on the synthesis of the prodrug of radiopharmaceutica l. About 85 % of malignacy express positive for telomer- ase. It aims to search for a kind of new compound , which can restrain telomer- ase and therapy tumo r. In this work , a novel prodrug of radioiodopharmaceuti- calCC6H 4IPOClNH CCH 2 )6NH-Leu-Gly-Boc) had been designed and synthe- sized. Some important inter-mediates also had been synthesized. The compound had been analysed using E. 丘， 1 HNMRCD20 , 200 MHz) and ESI-MS. The results indicated that the synthesis was successful. C6H4IPOCINHCCH2)6NH- Leu-Gly-Boc was synthesised from liquid phase instead of trational state phase , which would reduce the cost and improve the maneuverability. Key words: Prodrug of radiopharmaceutical , Phenol , Liquid phase 203 引 放射性棋标记的单克隆抗体(McAb) 作为一种靶向药物具有许多的优点，但是单克隆 抗体作为诊