3－[4－（4－[^18F]氟苯甲基）哌嗪－1－基]－甲基－1H－吡咯并[2，3－b]吡啶的放射化学合成

L-750,667是具有高亲和性(Ki＝0.51 nmol/L)的D4受体选择性配体,采用一锅法用氟[18F]化物放射化学合成了L-750,667的类似物3-[4-(4-[18F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶.4-氟[18F]苯甲醛是由无载体的[18F]F-与标记前体4-三甲基铵苯甲醛-三氟甲基磺酸盐在DMSO中反应获得.在同一容器中,4-氟[18F]苯甲醛和3-(哌嗪-1-基)甲基-1H-吡咯并[2,3-b]吡啶完成胺烷基化反应得到产物.产物的纯化使用HPLC,产物保留时间tR＝9.4min.在同一条件下,确定产物的放化纯度.放化产率为12.0%,放化纯度＞98%,比活度高于37GBq/μmol,全部合成时间(包括高效液相分离)为73min.制备的产物可作为潜在的多巴胺D4受体正电子发射断层(PET)显像剂.     

3-[4-(4-[~(18)F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶的放射化学合成

L-750,667是具有高亲和性(Ki= 0.51 nmol/L)的D4受体选择性配体,采用一锅法用氟[18F]化物放射化学合成了L-750,667的类似物:3-[4-(4-[18F]氟苯甲基)哌嗪-1-基]-甲基-1H-吡咯并[2,3-b]吡啶。4-氟[18F]苯甲醛是由无载体的 [18F]F-与标记前体4-三甲基铵苯甲醛-三氟甲基磺酸盐在DMSO中反应获得。在同一容器中,4-氟[18F]苯甲醛和3-(哌嗪-1-基)甲基-1H-吡咯并[2,3-b]吡啶完成胺烷基化反应得到产物。产物的纯化使用HPLC,产物保留时间tR=9.4min。在同一条件下,确定产物的放化纯度。放化产率为12.0%,放化纯度>98%,比活度高于37GBq/μmol,全部合成时间(包括高效液相分离)为73min。制备的产物可作为潜在的多巴胺D4受体正电子发射断层(PET)显像剂。     

N-琥珀酰亚胺4-[18F]氟苯甲酸酯的合成

合成了18F标记多肽和蛋白类药物中常用的中间体N-琥珀酰亚胺-4-[18F]氟苯甲酸酯([18F]SFB).由于[18F]SFB能和生物分子结合达到较高的标记率以及具有较好的体内稳定性,成为一种最适宜的氟-18标记试剂.本工作首先合成标记前体乙基-4-三甲胺苯甲酸酯-三氟磺酸盐,接下来经三步放射合成,然后经Sep-Pak C18柱分离可得[18F]SFB,并对第一步的18F标记反应进行了优化.合成时间约1 h;放化产率约50%;经放射性TLC和HPLC分析,放化纯度大于98%.     

6-[~(18)F]氟-L-多巴的合成

以硝基藜芦醛为原料 ,采用亲核取代合成法 ,利用手性相转移催化烷基化等多步反应制备了6 [18F]氟 L 多巴 (18FDOPA) ,并用手性流动相和反相C18柱的HPLC法测定对映纯度。结果表明 ,18FDOPA总的合成时间少于 12 0min ,经衰减校正后总放化产额约为 6 3% ,对映纯度和放化纯度分别大于 95 %和 99%     

苯甲酰胺类多巴胺D2受体显像剂18F-FSABZM的合成和标记

将5-硝基取代苯甲酰胺类化合物经硝基还原、N-双羟乙基化、甲磺酰化等反应制备氟标记前体,用K222催化进行氟标记,合成了(S)-N-[(1-乙基-2-比咯烷基)甲基]-5-[N-(2-[18F]氟乙基)-N-甲基磺酰基]胺基-2-甲氧基苯甲酰胺(S)-N-[(1-ethyl-2-pyrrolidinyl)methyl]-5-[N-(2-[18F]fluoroethyl)-N-methylsulfonyl]amino-2-methoxy-benzamide,18F-FSABZM).标记前体、冷标记产物和各步合成中间体均经过核磁共振和质谱确证.结果显示,经HPLC检测,标记率为12%-15%,合成及纯化时间80-90 min,纯化后放化纯度大于97%,稳定性好.     

6-[~(18)F]氟-L-多巴的合成

以硝基藜芦醛为原料,采用亲核取代合成法,利用手性相转移催化烷基化等多步反应制备了6-[^18F]氟-L-多巴（^18FDOPA）,并用手性流动相和反相C18柱的HPLC法测定对映纯度。结果表明,^18FDOPA总的合成时间少于120min,经衰减校正后总放化产额约为6.3%,对映纯度和放化纯度分别大于95%和99%。     

~(18)F-FMTP的放射化学合成

8 甲氧基 3 (4 氟苄基) 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮(FMTP)作为选择性多巴胺D4受体拮抗剂显示出高的亲和性和选择性(与D4受体的结合常数Ki=4.3nmol/L,与D2受体的结合常数Ki>5800nmol/L)。文章采用三氟甲基磺酸 4 三甲基铵苯甲醛为前体,完成了18F标记的亲核取代反应,用18F标记的中间体同8 甲氧基 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮完成胺烷基化反应,得到目标产物8 甲氧基 3 (4 [18F]氟苄基) 1,2,3,4 四氢苯并吡喃[3,4 c]吡啶 5 酮(18F FMTP)。产物的总合成时间(包括高效液相纯化)为110min,放化产率为19.5%,放化纯度大于98%,比活度高于37GBq/μmol。     

1-[~(18)F]氟代乙基-L-色氨酸的半自动化合成

设计并合成了一种新型氟标记氨基酸类似物1-[18F]氟代乙基-L-色氨酸(1-[18F]FETrp)。以色氨酸为原料,采用有机合成法经过七步反应,合成了标准品1-[19F]FETrp;使用氟多功能模块,采用亲核取代法,将放射化学标记自动化。经过对1-[19F]FETrp自动化合成条件的摸索,最后采用二锅法合成了1-[18F]FE-Trp。1-[18F]FETrp的放化产率为1.5%,合成时间50 min;由于放化产率过低,今后需改变条件或者寻找新的合成路线以提高产率,以期为临床区分炎症和肿瘤提供新的PET显像剂。     

6-[18F]氟-L-多巴的质量控制

6－[^18F]氟－L－多巴（^18FDOPA,I）为L－多巴的类似物，是研究大脑突触前多巴胺能神经功能的正电子显像剂，为在临床上安全有效地使用^18FDOPA，对合成的^18FDOPA进行了较系统的质量控制研究，并建立了手性流动相HPLC法测定^18FDOPA对映纯度，合成的^18FDOPA各项质控指标符合药典的要求，本研究为研制新型PET显像剂提供了质量控制模型，为测定^18FDOPA和其他L－型氨基酸的对映纯度提供了廉价而实用的方法。     

5-羟色胺受体显像剂18F-MPPF的合成和标记

报道了5-羟色胺(5—HTlA)受体显像剂4-[^18F]氟—N-[2-[1-(2-甲氧基苯基)-1—哌嗪基乙基]-N—2吡啶基-苯甲酰胺(^18F-fluor-N-[2-[1-(2-methoxyphenyl)]-1-PiPenninyl]ethyl—N-2-Pridinyl—benzaInide,^18F-MPPF)的合成和标记。标记前体MPPN02和各步合成中间体均由红外、元素分析、核磁共振和质谱确证;采用两种加热方法进行氟代亲核置换标记反应。结果显示,微波法标记的放化产额(34％—50％,n＝10)明显比油浴加热标记法(8％一24％,n＝10)高,反应时间(40-50min)也比油浴加热标记法(70—40min)短,用TLC和HPLC检测放射化学纯度(RCP)均大于95％,可用于临床前研究。     

Preparation of Zn/TiO2 powder and its photocatalytic performance for oxidation of P-nitrophenol

Zn-doped TiO2 catalysts were prepared using a sol-gel method and characterized by XPS,UV-Vis, BET, XRD in this study. Under the irradiation of simulant sunlight, the photocatalytic activity for the degradation of p-nitrophenol was studied too. After irradiation for 2.5 h, the degradation percentage of p-nitrophenol could rise to more than 80 %. The results showed that the spectrum absorption band edge of Zn/TiO2 powder does not broaden obviously comparing with pure TiO2 powder. Zinc exists as Zn （11）. When calcined at 973 K, there is a new phase as ZnTiO3 in Zn/TiO2 catalyst. The order of photocatalytic activity of Zn/TiO2 catalysts calcined at different temperatures for p-nitrophenol is 773 K 〉 673 K 〉 873 K 〉 573 K 〉 973 K and the photocatalytic activity of Zn/TiO2 catalyst calcined at 773 K is better than TiO2 catalysts heated at the same temperature, and outclasses that of commercial TiO2 catalyst. It also showed that the photocatalytic degradation of p-nitrophenol follows first-order kinetics under the irradiation of simulant sunlight.     

Current status of radiation therapy for prostate cancer

Radiotherapy for the treatment of prostate cancer has been extensively explored in the past. Along with the comprehensive understanding of the biology of prostate cancer and rapid advances in terms of technology, the out- come of treatment for the patients with prostate cancer has improved. The authors review radiotherapy as the primary treatment for the disease, with particular emphasis on the technological advances from both the radiobiological and radiophysics aspects. Nonconventional fractionated irradiation like hyper- or hypo-fractionation has been imple- mented in the clinic, the final results still need to be confirmed in the future. Technological advances like IMRT, IGRT, in the last two decades have significantly improved the delivery of external radiotherapy to the prostate. This has re- sulted in an overall increase in the total dose that can be safely delivered to the prostate, which has led to modest im- provements in the biochemical outcome. However, establishing the standard therapy for prostate cancer remains con- troversial. It is hoped that the next decades will bring continued advances in the development of biologicals that will further improve current clinical outcomes.     

The control system for SSRF injection and extraction

This paper introduces the injection and extraction control system design for SSRF,which is a distributed control system aimed at stability and reliability of the pulse power supplies,PPS(Personnel Protection System)and MPS(Machine Protection System).The hardware environment is mainly based on PLC(Programmable Logic Con- troller),and ARM(Advanced RISC Machine)is also applied for studying stability of the power supplies.WinCC and EPICS(Experimental Physics and Industrial Control System)have been selected as the platforms of SCADA(Super- visory Control and Data Acquisition).For unifying the interfacing to the control computer,all front-end equipments are connected via Industrial Ethemet.     

水平管内含空气蒸汽强制对流冷凝换热模型研究

为研究含空气蒸汽在水平管内强制对流冷凝换热特性,基于对传热传质过程的分析,建立了管内为环状流与波状流条件下的流动冷凝换热模型。从潜热、显热和液膜3个环节对整个换热过程进行建模,最终得到计算局部冷凝换热系数的理论关系式。模型预测结果与实验数据的对比表明,二者相对偏差在±20%以内,验证了该换热模型的准确性与适用性。通过进一步的研究发现：从换热管入口至出口,随着冷凝的进行,管内换热主要热阻由液膜热阻向气液界面的凝结热阻转变;主流气体对流换热过程基本可忽略。     

Investigations on landmine detection by BF3 detector

Experiments were carried out to investigate the possible use of neutron backscattering for the detection of polyethylene (PE) sample buried in the soil. In detection of landmine by neutrons, the neutron detector and its shield play an important role. In this paper, the effects of graphite, heavy water, polyethylene and boric acid moderators on the flux of back scattered neutrons were investigated. We have also experimentally verified the effect of BF3 detector shield and obtained good agreement with theory.     

Web Services interface of SSRF archive data analysis system

Accelerator database stores various static parameters and real-time data of accelerator. SSRF (Shanghai Synchrotron Radiation Facility) adopts relational database to save the data. We developed a data retrieval system based on XML Web Services for accessing the archive data. It includes a bottom layer interface and an interface applicable for accelerator physics. Client samples exemplifying how to consume the interface are given. The users can browse, retrieve and plot data by the client samples. Also, we give a method to test its stability. The test result and performance are described.     

Assessment of radioactivity levels in some oil samples from the western desert, Egypt

Distributions of natural gamma-emitting radionuclides were determined in 93 oil samples collected from some petroleum fields in the western desert of Egypt. The radioisotope activities in the area under investigation lay in the range of (21 ± 4) to (38 ± 13) Bq?L-1 for 226Ra, (9 ± 2) to (15 ± 5) Bq?L-1 for 232Th, and (154 ± 28) to (303 ± 54) Bq?L-1 for 40K. The mean values were 27, 12, and 201 Bq?L-1, respectively. Among oils, variations in radionuclide ac- tivities could be on account of differences in TDS, HCO3, and Ba, with high or low pH. In this environment, oil prop- erties differently affected the mobilization of natural radionuclides. The range of 226Ra variation had been compared with available data from other countries. The calculated absorbed dose rate ranged from 22.33 to 32.66 nGy?h-1 in lo- cation (B) and (E) respectively, which was less than the accepted value.     

Preparation and properties of 117m Sn(IV)-TTHMP in in-vitro and in small animals

In this work,TTHMP was synthesized and labelled with 117m Sn.The preparation conditions,stability and lipophilicity of 117m Sn(IV)-TTHMP were investigated.Biodistribution of the complex in rabbits and mice was studied.It was found that the quantity of TTHMP and pH value of the prepararion solution had vital effects on the labeling yield of 117m Sn(IV)-TTHMP.It was also found that 117m Sn(IV)-TTHMP was hydrophilic and stable at room temperature and 37℃ in open air 117m Sn(IV)-TTHMP showed unexpectedly high bone uptake and bone-to-blood ratio in the animals.This made it potentially useful as an reagent for skeletal scintigraphy and radiotherapy of bone tumors.     

The role of AGFA high-energy CR in the calibration and quality control of multileaf collimators （MLC）

Linear accelerators equipped with multileaf collimators （MLC） are becoming more common and are widely used in the intensity-modulated radiotherapy （IMRT）. There is an imperative need to ensure the commissioning specification of the linear accelerators for the sake of quality assurance （QA） and quality control （QC）. This paper is aimed to investigate the role of AGFA high-energy CR （Computed Radiography） in calibrating dynamic multileaf collimators and evaluating the accuracy of the leaf position. The result shows that AGFA high-energy CR can easily and conveniently be used to calibrate MLC and verify its position. Hence, the application of AGFA high-energy CR is proved to be an accurate and time-saving method for routine MLC QC, especially when MLC calibration adjustments are required.     

Gamma radiation levels in the ambient environment of the QNPP Base

Monitoring results of gamma dose rate level in 1992～2004 in the ambient environment of the Qinshan Nuclear Power Plants(QNPP)Base,the northeast of Zhejiang Province,are reported in this paper.It is shown that the gamma dose rate of five monitoring sites of 2.5 km to QNPP Base is 84～113 nGy/h,with an average of 96 nGy/h in the 13 years.The average value is close to the background level of 93 nGy/h prior to operation of the QNPP Base,and is lower than the monitoring result of 101 nGy/h at the reference site in Hangzhou City.Within 50 km from the QNPP Base,the cumulative dose rate of the thermoluminescent dosimeter(TLD)is 90 nGy/h,which is lower than the back- ground level of 111 nGy/h.