尽管现代医学水平不断提高，但肿瘤仍然是严重危害人类健康的疾病之一，如何能够快速准确地获得早期肿瘤组织的病理和生理信息对肿瘤的有效治疗起着举足轻重的作用。近年来，随着核医学显像仪器的快速发展和肿瘤放射性药物的研究和开发利用，放射性核素标记的肿瘤显像剂对肿瘤的早期诊断、良恶性鉴别、分期、分级及预后评估等方面显示了其独特的优势。表皮生长因子受体是酪氨酸激酶受中表皮生长因子（EGF）家族的一员。EGFR酪氨酸激酶（EGFR-TK）抑制剂可与三磷酸腺苷竞争性结合胞内的ATP结合位点，通过抑制酪氨酸激酶，从而阻断受体催化活性，进而阻断下游信号传导。酪氨酸激酶抑制剂吉非替尼(Gefitinib)和厄洛替尼(Erlotinib)已广泛用于治疗非小细胞肺癌（NSCLC），坦度替尼（Tandutinib）用于白血病和晚期骨髓增生的Ⅱ期临床治疗。因为EGFR在肿瘤细胞中的高密度表达，使4-苯胺喹唑啉类的放射性标记化合物具有成为肿瘤显像剂的潜力。用EGFR酪氨酸激酶抑制剂作为EGFR过度表达肿瘤的放射性分子示踪剂成为核医学界的研究热点。本论文以3,4-二甲氧基苯甲酸为原料，经过多步反应得到喹唑啉环，并在保留喹唑啉类抗肿瘤药物有效集团的前提下，以喹唑啉母核为基础，利用电子等排取代和药物拼合原理设计合成并标记了5个目标化合物，这些新的化合物均经过IR、1HNMR、13CNMR、MS的鉴定，19F取代产物亦有19FNMR确认结构。除此之外还对放射性标记化合物进行了一系列的生物活性测试。实验结果显示，新标记化合物在体内和体外均显示了良好的稳定性。由小鼠体内分布数据可以看出，新标记化合物在肿瘤中都有一定的放射性积累，且血清除速率较高。其中18F标记的三个喹唑啉类化合物都有优于18F-FDG的肿瘤绝对摄取量和肿/肉值，尤其16b在60min时肿/肉值值达到7.70，优于现今最好的肿瘤显像剂18F-FDG，有利于呈现清晰的显像效果。综合考虑新标记的五个化合物的各方面性能，16b在血清除速率、肿瘤的放射积累量以及靶/非靶值都显示了较好的活性，有成为肿瘤显像剂的巨大潜力，有待于进一步的药物开发和临床研究。目前广泛用于喹唑啉标记的方法需时过长，且标记率不高，本论文探索了喹唑啉类化合物的多种标记方法并确定了合适的标记路线，为喹唑啉类显像剂的广泛研究和应用开辟了一条新的途径。综上所述，这些研究的完成丰富了放射性肿瘤显像剂的研究内容，为寻找新型的特异性的肿瘤显像剂的研究提供了一个新的思路。

While the rapid development of modern medical science, cancer is still one of the diseases which were serious hazard to human health. How to obtain information on the pathophysiology of tumor tissue quickly and accurately for effective treatment of tumors plays an important role. In recent years, with the development of nuclear medicine imaging equipment and further radiopharmaceuticals cancer research, radionuclide tumor imaging agents show their advantages in early diagnosis of cancer, identification of benign and malignant, stage, grade, and clinical prediction.EGFR is a member of the epidermal growth factor (EGF) family of tyrosine kinase receptors (which also includes ErbB2, ErbB3 and ErbB42). Ligand binding to the extracellular domain of the receptor results in the activation of the receptor. The activated receptor can dimerize with other EGFRs followed by phosphorylation of tyrosine residueson the receptors. This active conformation makes it possible for TK domain of the receptors both to bind ATP and to transphosphorylate each other. Receptor autophosphorylation on tyrosine residues both enhances the activity of kinases and provides docking sites for downstream signal transduction molecules that habor SH2 or PTB domains. These interaction activate signal transduction pathways, which ultimately lead to multiple cellular processes, such as proliferation, differentiation, apotosis, angiogenesis, cell adhesion and movement. Tyrosine kinases inhibitors erlotinib and gefitinib have been launched for the treatment of non-small-cell lung cancer (NSCLC) and tandutinib (MLN-518) is in phase Ⅱ clinical trials for myeloid leukemia (ML) or advanced myelodysplasia (MDS).Because of the high-density expression of the epidermal growth factor in cancer cells, the radiolabeled 4-aminoquinazoline derivatives have the potential to become tumor imaging agents. There has been a growing interest in the use of EGFR-TK inhibitors as radiotracers for molecular imaging of EGFR over expressing tumors via nuclear medicine modalities such as SPCET and PET.Several novel labeled precursors were designed and synthesized based on the structure of 4-aminoquinazolines in this paper. The structure of all novel product and intermediates were confirmed by IR, 1HNMR, 13CNMR, MS and 19FNMR which was included for 19F substitution product. Moreover, a series of experiments were carried out in order to evaluate the bioactivity of the complexes. Experimental results reveal that the new labeled compounds have shown good stability in vivo and in vitro. Bio distribution data shows that the new labeled compounds in tumors have a certain accumulation of radioactivity, and the blood clearance rate is higher. The absolute tumor uptake and tumor/ muscle value of the three 18F labeled quinazoline compounds are higher than 18F-FDG. Especially, the tumor uptake of 16b in 60min reached 2.98% ID/g, tumor / muscle value reached 7.70, better than 18F-FDG which is the current best imaging agent . Considering all aspects of the new five compounds, 16b have shown good activity in the blood clearance rate ,tumor accumulation of the radiation and T/M value, it is a potential tumor imaging agent to be further researches。This paper explored several labeled methods of quinazoline compounds，and then identified the appropriate method, which has opened up a new way for quinazoline extensive research and application.These studies enriched the research of tumor imaging agents, provided a new direction for the tumor imaging agent research. Further researches of the radiolabeled 4-aminoquinazoline derivatives were required.