β-榄香烯三羰基铼衍生物的放射化学合成

本文报道了β-榄香烯三羰基铼衍生物的合成及其同位素188Re标记.标记配体由β-榄香烯与双功能螯合剂二(2-吡啶甲基)-胺反应制得.标记产物直接由配体与fac-[188Re(CO)3(H2O)3] 制得,并经反向HPLC分离纯化.结果显示,标记配体收率为64%,标记产物放化产率40%,经HPLC分离后放化纯度达到95%以上.表明该法简单易行,其标记化合物有可能发展成为一种新的放射性药物.     

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.     

3-氨-1-羟丙基-1,1-二膦酸盐的131I标记化合物的合成及其初步动物实验

合成了3-氨-1-羟丙基-1,1-二膦酸二钠水合物(ABP)配体,并以5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯(SPC)为双功能偶联剂,进行了131I标记的研究.其标记率大于64%,放化纯度大于99%.室温下,标记产物放置72 h后,放化纯度仍大于98.8%.初步动物实验结果表明,标记产物131I-SIPC-ABP对小鼠骨骼具有明显的亲和力,具有较高的体内外稳定性.     

3-三甲基硅苄胍的合成及其125I标记

以3-溴甲苯为起始物，通过5步反应合成可用于放射性碘（砹）标记的3-三甲基硅苄胍，并用核磁共振（NMR）、质谱（MS）、高效液相（HPLC）等对产物进行了表征。以此化合物为前体，对其进行了¹²⁵I标记。¹²⁵I MIBG的标记率达66.7%，放化纯度＞98%。标记物在室温下放置3d后，放化纯度无明显变化，表明¹²⁵I MIBG具有较高的体外稳定性。     

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%.     

双功能偶联剂5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯的优化合成及其碘标记

为了改善碘标记生物分子在体内的脱碘问题,在无水无氧条件下合成了碘标记前体5-(三正丁基锡)-3-吡啶甲酸-N-琥珀酰亚胺酯（SPC）,并优化了合成条件,产率达到45%,并用核磁共振、质谱法进行了表征。在此基础上,合成了5-碘-3-吡啶甲酸-N-琥珀酰亚胺酯（SIPC）。对标记前体SPC的¹²⁵I 标记条件进行了摸索,最终标记率达到80%以上,经高效液相色谱（HPLC）分离后,放化纯度达到97％。标记后的¹²⁵I-SIPC在4℃保存24h,放化纯度仍在92％以上,稳定性良好。     

一种烟碱乙酰胆碱受体(nAChRs)显像前体化合物的合成与125I标记研究

本文介绍一种可用于125/123I标记的A-85380类前体化合物--(S)-5-(三丁基锡烷基)-3-[[1-(叔丁氧基羰基)-2-甲氧基]氮杂环丁基]吡啶的设计、合成及125I标记研究.实验以2-糠胺和(S)-氮杂环丁基甲酸为起始物,先合成(S)-5-(三丁基锡烷基)-3-[[1-(叔丁氧基羰基)-2-氮杂环丁基]甲氧基]吡啶前体化合物,再用125I标记,制得5-[125I]I-A-85380.整个放射性标记的时间为50-55min,标记率大于30%.5-[125I]I-A-85380在室温下放置3天,其放化纯度仍在95%以上,表明其在体外具有较高的稳定性.     

肿瘤增殖显像剂18F－FLT的合成和标记

为制备肿瘤增殖显像剂3'-脱氧-3'-氟胸腺嘧啶脱氧核苷(3'-deoxy-3'-fluorothymidine, 18F-FLT),合成了标记前体3-N-t-叔丁氧羰基-1-[5'-O-(4, 4'-二甲氧基三苯甲基)-2'-脱氧-3'-O-(4-硝基苯磺酰基-β-1)-苏戊呋喃糖]胸腺嘧啶脱氧核苷(N-BOC-FLT)并进行了标记.标记前体和各步合成中间体均经红外、核磁共振和质谱确证;于120 ℃进行亲核氟化反应,标记率为(35.2±5.8)%(经校正,n=2),用TLC和HPLC检测其放化纯度(RCP)大于95%,可满足临床研究的要求.     

[20-3H]佛波醇-12-肉豆蔻酯-13-乙酯的合成

用MnO2将佛波醇-12-肉豆蔻酯-13-乙酯氧化，然后利用新制的NaB^3H4氚化还原合成[20-^3H]佛波醇-12-肉豆蔻酯-13-乙酯。所得产物经HPLC纯化后放化纯度〉98％，其比活度达0．654TBq／g。纯化产物在-20℃放置90天仍保持稳定。本法简单易行，标记过程中也不产生异构体。     

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.     

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.     

有效探测面积大于1000 cm2的正比计数器测量系统性能测试

为对自制的活性面积高达1 000 cm²的大面积源进行表面发射率定值,同时作为现有2πα、2πβ表面发射率标准装置能力的扩充,研制了一套内置式大面积2π多丝正比计数器测量系统,并利用活性区直径为8 mm的²⁴¹Am点源及活性区面积为10 cm×15 cm的大面积²⁴¹Am和⁹⁰Sr-⁹⁰Y源对其进行计量学性能测试。结果表明：计数器内计数响应均匀性优于±0.4%,有效探测面积达1 400 cm²;所得²⁴¹Am源高压坪曲线的坪长为1 400 V,坪斜为0.27%/100 V,坪区内计数变化为0.87%;⁹⁰Sr-⁹⁰Y源高压坪曲线的坪长为300 V,坪斜为0.75%/100 V,坪区内计数变化为0.80%;10次测量重复性好于0.4%,8 h内短期稳定性好于0.3%,1 a内长期稳定性好于0.8%。     

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.