论文部分内容阅读
以Cyclofenil为原料,合成得到一系列氟乙氧基衍生物.通过受体结合实验,筛选得到一个对雌激素受体(ER)具有高特异性和高相对亲和力(RBA)的化合物Penta-Cyclofenil-FEt.通过实验的优化设计,合成得到相应的氟标记前体,产物通过IR,UV,1H NMR,19F NMR或ESI-HRMS进行了表征.在冷试条件下,得到了冷氟取代参比化合物.在热试验条件下,得到F-18标记产物.此类非甾体雌激素受体分子探针的合成,为PET(positron emission tomography)显像雌激素受体β从而评估乳腺癌的恶化程度奠定了基础.
Cyclofenil was used as a starting material to synthesize a series of fluoroethoxy derivatives.According to receptor binding experiments, a compound with high specificity and high relative affinity (RBA) to estrogen receptor (ER) was screened.Penta-Cyclofenil- FEt. The corresponding fluorine-labeled precursors were synthesized through the optimization of experimental design and the products were characterized by IR, UV, 1H NMR, 19F NMR or ESI-HRMS. The F-18 labeled product was obtained under thermal test conditions.The synthesis of such non-steroidal estrogen receptor molecular probes was used to visualize the estrogen receptor beta by positron emission tomography (PET) to assess the degree of deterioration of breast cancer Foundation.