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1.
羟基吡啶酮类化合物是一类新型的铁螯合剂,我们以糠醛为起始原料,与溴乙烷的格氏试剂加成,水解得α-乙基呋喃甲醇(A);A经氯氧化重排反应制得2-乙基-3-羟基吡喃-4-酮(B);B与胺反应合成出1-烷基-2-乙基-3-羟基吡啶-4-酮。产物结构均经IR,NMR光谱鉴定。  相似文献   

2.
以POLYGEN软件中的CHARMm程序和集团坐标轮换法,对6个化合物的结构进行计算机分子模拟,根据所得化合物的能量最低构象,计算了键合能、电子总能量、偶极矩、胺基氮原子电荷以及氧原子电荷等值并作为结构参数对反应的反应热进行估算,同时对β-苯乙胺N-取代反应中的重排反应(反应式(1))进行机理研究,结果认为重排产物N-(2-苯乙基)N-(2-羟乙基)-对硝基苯胺4是由N-(2-苯乙基)-2-(对硝基苯氧基)乙胺3经分子内亲核取代反应所得,此反应可能为Smiles重排反应。  相似文献   

3.
以POLYGEN软件中的CHARMm程序和集团坐标轮换法,对6个化合和折结构进行计算机分子模拟,根据所得化合物的能量最低构象,计算了键合能,电子总能量,偶极矩,胺基氮原子电荷以及氧原子电荷等值并作为结构参数对反应的反应热进行估算,同时对β-苯乙胺N-取代反应中的重排反应(反应式(1)进行机理研究,结果认为重排产物N-(2-苯乙基)N-(2-羟乙基)-对硝基苯胺4是由N-(2-苯乙基)-2-(对硝基  相似文献   

4.
应用一氯二乙基铝和苄基氯催化剂体系进行了丁苯橡胶的阳离子环化反应。研究了反应温度、苄基氯/一氯二乙基铝比例、溶剂、原胶浓度对环化的影响。发现通过控制苄基氯/一氯二乙基铝比,可在高温(120℃)、高原胶浓度(2~4%w/v)下进行丁苯橡胶的环化,制得特性粘度较原胶有大幅度降低,可溶性无凝胶的环化丁苯胶。通过对红外光谱、^1H-NMR谱初步解析,证实了环化反应的发生。  相似文献   

5.
报道通过延伸方法解决季戊四醇(1)及三羟甲基氨甲烷(2)末端羟基立体位阻的方法。(1)和(2)末端羟基经氰乙基化、醇解和还原等步骤制得标题化合物四(ω-羟丙氧甲基)甲烷(3)及三(ω-羟丙氧甲基)氨甲烷(4),并合成9个衍生物,以摸索(3)和(4)的酰化、醚化及氯化等反应条件。所合成的化合物(3~13)及(15)均未见文献报道,其结构经IR、1H-NMR和元素分析确证。标题化合物可作为小分子多功能桥试剂,以增大载体的载药量。  相似文献   

6.
报道通过延伸方法解决季戊四醇(1)及三羟甲基氨甲烷(2)末端羟基立体位阻的方法。(1)和(2)末端羟基经氰乙基化、醇解和还原等步骤制得标题化合物四(ω-羟丙氧甲基)甲烷(3)及三(ω-羟丙氧甲基)氨甲烷(4),并合成9个衍生物,以摸索(3)和(4)的酰化、醚化及氯化等反应条件,所合成的化合物(3-13)及(15)均未见文献报道,其结构经IR、^1H-NMR和元素分析确证。标题化合物可作为小分子多功  相似文献   

7.
β-苯乙胺N-取代反应中的重排反应   总被引:4,自引:0,他引:4  
合成了N-(对硝基苯氧乙基)β-苯乙胺(3),同时分离到重排产物N-(2-苯乙基)-N-(2-羟乙基)-对硝基苯胺(4),推测可能是一分子内亲核取代反应。  相似文献   

8.
目的合成5-氟尿嘧啶类衍生物。方法用三氯锗基丙酚氯与2,4-二(三甲基硅氧基)-5-氟尿嘧啶反应得到1-(三氯锗基丙酰基)-5-氟尿嘧啶(Ⅰ).(Ⅰ)经水解即得到其水解产物β-N1-(5-氟尿嘧啶)甲酰基乙基锗倍半氧化物(Ⅱ)。结果合成了化合物(Ⅰ)和(Ⅱ)。它们的结构由IR,1HNMR及元素分析确证。  相似文献   

9.
以Pd/C为催化剂,考察了温度、压力、溶剂、溶剂量、溶液pH值、搅拌速度及反应原料对m-β-羟乙基砜硝基苯催化加氢制,m-β-羟乙基苯胺的影响。表明以自制的w=0.02Pd/C为经剂,经提纯的工厂中间体m-β-羟乙基砜硝基苯为原料,在65℃、3.5MPa、乙醇为溶剂、原料:乙醇:催化剂=1:1:0.05(m/m)、溶液pH值7~8、搅拌速度800r/mih的条件下反应2h,反应得率可达99.7%^  相似文献   

10.
探讨3-取代氨基乙基-4-甲基-7-羟基香豆素衍生物合成的简便方法。方法 间苯二酚和2-(β-二乙氨基惭基乙酰乙酸乙酯经Pechmann反应得3-(β-二乙氨基)乙基-4-甲基-7-羟基香豆素,再经Williamson反应,生成7-羟基香豆素的衍生物。  相似文献   

11.
Objective: To evaluatel the value of D-dimers in patients with acute aortic dissection (AAD). Methods: This study consisted of 16 patients with AAD and 27 non-AAD patients. Serum D-dimets were measured by Sta-Liatest D-DI immunoturbidimetric assay. Results: D-dimer level was higher (P < 0.001) in patients with AAD(7.91 ± 5.52 μg/ml) than that in non- AAD group(1.57±1.24 μg/ml). D-dimer was positive (>0.4 μg/ml) in all patients with AAD and in 10 control group patients (37%). Among patients with acute AAD, D-dimers tended to be higher in Stanford A than in Stanford B (8.67 ± 4.31 μg/ml vs. 3.24±1.27 μg/ml, P <0.01). D-dimer values tended to be higher in more extended disease(3.84 ± 1.65 μg/ml, 8.57 ± 3.58 μg/ml and 11.87 ± 5.69 μg/ml in thoracic aorta, thoracic and abdominal aorta, thoracic and abdominal aorta and iliacal arteries, respectively, P < 0.05 for both 8.57 ± 3.58 and 11.87 ± 5.69 vs. 3.84 ± 1.65 ). Including the control group into the analysis, we found a sensitivity of 100%, a negative predictive value of 100%, and a specificity of 66% and a positive predictive value of 64% for D-dimer in diagnosis of AAD in our patients with suspected AAD. Conclusion: D-dimer was elevated in patients with AAD. A negative D-dimer test result could be useful in excluding AAD.  相似文献   

12.
Objective: To set up a simple and reliable rat model of combined liver-kidney transplantation. Methods: SD rats served as both donors and recipients. 4℃ sodium lactate Ringer's was infused from portal veins to donated livers,and from abdominal aorta to donated kidneys, respectively. Anastomosis of the portal vein and the inferior vena cava (IVC) inferior to the right kidney between the graft and the recipient was performed by a double cuff method, then the superior hepatic vena cava with suture. A patch of donated renal artery was anastomosed to the recipient abdominal aorta. The urethra and bile duct were reconstructed with a simple inside bracket. Results: Among 65 cases of combined liver-kidney transplantation, the success rate in the late 40 cases was 77.5%. The function of the grafted liver and kidney remained normal. Conclusion: This rat model of combined liver-kidney transplantation can be established in common laboratory conditions with high success rate and meet the needs of renal transplantation experiment.  相似文献   

13.
Objective To observe blood pressure change with age in salt-sensitive teenagers whose salt sensitivity were determined by repeated testing.Methods Salt sensitivity was determined through intravenous infusion of normal saline combined with volume-depletion by oral diuretic furosemide in 55 teenagers. After five years, salt sensitivity was re-examined and subject blood pressure was followed up. Blood pressure changes in salt-sensitive teenagers were compared to that of non-salt sensitive teenagers over five years.Results After 5 years, the repetition rate of salt sensitivity determined by intravenous saline loading is 92.7%. In teenagers with salt sensitivity on the baseline, both the systolic blood pressure increments and increment rates were much higher than non-salt sensitive teenagers (12.7±12.1 mmHg vs. 2.8±5.2 mmHg, P< 0.01; 12.2%± 12.0% vs. 2.5% ±4.4%, P< 0.001,respectively). There was a similar trend for diastolic blood pressure (8.4 ± 6.4 mmHg vs. 3.7 ± 6.4 mmHg, P = 0.052; 13.2% ±10.6 % vs. 6.8%± 10.1%, P = 0.053, respectively).Conclusions Salt sensitivity determined by intravenous saline loading showed good reproducibility. Blood pressure increments with age were much higher in salt-sensitive teenagers than non-salt sensitive teenagers, especially in terms of systolic blood pressure.  相似文献   

14.
目的:评价使用安心颗粒对急诊经皮冠状动脉介入术(PPCI)术后生活质量的影响.方法:将160例接受PPCI的急性ST段抬高型心肌梗死患者随机分为安心颗粒组(术前顿服安心颗粒8.8g,术后安心颗粒4.4 g/次,每日2次)和对照组(仅接受基础药物治疗).所有患者均服用阿司匹林、氯吡格雷和阿托伐他汀.分别在入院时、出院前1d、出院后180 d时,应用心肌梗死多维度量表(MIDAS)、中文版SF-36评价量表对患者生活质量评分.并观察术后30 d以内的出血并发症、血小板减少症发生情况.结果:入院时和出院前1d,两组患者的心肌梗死MIDAS、SF-36量表评分比较无差异(P>0.05);出院后180 d时,与对照组比较,安心颗粒组MIDAS、SF-36评分明显减低(P<0.05);组内与入院时比较,两组出院前1d、出院后180 d时,MIDAS、SF-36评分均降低(P<0.05).两组患者在随访期间均无大量出血、少量出血、重度和极重度血小板减少症发生,安心颗粒组有4例、对照组有7例发生不明显出血(P>0.05).两组发生轻度血小板减少症的患者数比较无差异(P>0.05).结论:PPCI使用安心颗粒,能改善急性ST段抬高型心肌梗死患者的生活质量,且不增加出血风险.  相似文献   

15.
Objective:To investigate the influences of urapidil and nicardipine on rabbit sinus function,atrio-ventricular node function and hemodynamics.Methods:Thirty-two Angora's rabbits were selected and randomly divided into four groups.U1 group:urapidil 0.25 mg/kg;U2 group:urapidil 0.5 mg/kg;N1 group:nicardipine 10 μg/kg;N2 group:nicardipine 20 μg/kg.All these medicine were administrated within 30 seconds.Measurements were taken before and after the administration of urapidil or nicardipine for the following data:mean blood pressure(MAP),heart rate(HR),sino-atrial conduction time(SACT),maximal sinoatrial recovery time(SNRTmax)corrected sinus node recovery time(CSNRT),index of sinus node recovery time(SNRTI),Wenckebach A-V conduction frequency (WB),and P-R interval.Results:Significant MAP and HR changes were identified in all of the four groups before and after administration of both urapidil and nicardipine.No significant changes could be found in the rest of the parameters.Intergroup analysis showed that SACT and CSNRT of N1 and N2 groups were shorter than those of the U2 group(P<0.01);the MAP decreased(P<0.01)and the HR increased drastically(P<0.01).Conclusions:Neither urapidil(0.25 mg/kg,0.5 mg/kg)nor nicardipine(10μg/kg,20μg/kg)has any significant influence on rabbit sinus function or rabbit atrio-ventricular node function.Nicardipine could be a better choice than urapidil for parafunctional sinus node patients.  相似文献   

16.
Objective:To investigate the gene expression of osteoprotegerin(OPG) and osteoclast differentiation factor(ODF) in the bone tissue of patients with hip fracture due to osteoporosis. Methods:OPGmRNA and ODFmRNA in the bone tissue in 50 cases of osteoporosis sufferers(over 50 years old) with hip fracture(Observer Group) and 30 cases of hip facture sufferers with no osteoporosis(Control group) were analyzed with the Semi-Quantitative RT-PCR method. Results:The mRNA expressed of ODF, OPG were both high in the patients with hip fracture. In the control group, the expression of OPG mRNA was observed, while the expression of ODF mRNA was very slight. Conclusion:Aged patients contained all signals including OPG, ODF that are essential for inducing osteoclastogenesis and promoting bone resorption.  相似文献   

17.
Objective:To investigate the clinical features, pathological characteristics and immunophenotype of solid-pseudopapillary tumor of the pancreas(SPTP). Methods:Nine surgically treated cases of SPTP were retrospectively reviewed. Hematoxylin and Eosin(HE) staining and immunohistochemical staining were used to analyze all cases, and the general clinical data was collected. Results:Six patients were asymptomatic except for a palpable mass. Two patients complained of vague-epigastric pain. One patient appeared jaundice. The tumor was encapsulated and solid tissues alternately with cystic tissues. Histologically, the histological structure of solid portion was pseudopapillary with a fibrovascular core. Tumor cells were uniform and medium-sized which were arranged in sheets ets or nests or pseudopapillary patterns. Immunohistochemical studies demonstrated that SPTP proved positive in vimentin(9/9 cases), AAT(9/9 cases), NSE(9/9 cases), ACT(7/9 cases), CK20(2/9 cases), CgA(1/9 cases), S-100(3/gcases), PR(4/gcases), Syn(3/9 cases) and CD56(5/9cases), negative in CEA and ER. Conclusion:SPTP is a tumor predominantly occurring in young women frequently without special symptoms. This tumor has various characteristical histological patterns with different immunophenotype.  相似文献   

18.
Objective:To probe into the influence of changes of ovarian hormones on the pathogenesis of the specific sub-type premenstrual syndrome(PMS)and reveal partial microcosmic mechanisms of adverse flow of liver-qi.Methods:Estradiol(E2)and progesterone(P)levels in serum were determined at different phases of menstrual cycle by radioimmunoassay.Results:In the group of PMS with adverse flow of liver-qi.the secretive peak value Of E2 and P at the follicular phase significantly decreased,and the secretive peak value at the luteal phase did not come into being.Conclusions:Low E2 and P secretive peak at the follicular phase and absence of secretive peak at the luteal phase is one of the microcosmic mechanisms of PMS with adverse flow of liver-qi.One of the pathophysiologic mechanisms of specific sub-type PMS is probably the continuous low level of E2and P.  相似文献   

19.
Real-time three-dimensional echocardiography (RT3DE)is a new ultrasound technique that enables dynamic threedimensional visualization and quantification of the heart in real time. Investigation of feasibility and methodology of RT3DE in determining left ventricular (LV) and right ventricular (RV) volumes, RT3DE was performed in 35 normal adults using Philips SONOS 7500 system with a 2-4 MHz matrix array transducer. The 60°×60° "pyramid" volume database was obtained and analyzed on a TomTec echo workstation. Both LV and RV volumes were calculated with four 3DE methods (i.e. apical 2, 4, 8, and 16-plane) through manually tracing ventricular endocardial borders in end diastole and end systole. Stroke volumes were then calculated. LV volume was also measured by 2DE Simpson's rule using GE VIVID 7 ultrasound machine.  相似文献   

20.
Increasing maternal age is the only etiological factor unequivocally linked to Down's syndrome in humans. The occurrence rate of newborns with Down's syndrome is about 1/220 in women over 35 years old. However, the occurrence rate in embryos fertilized in vitro, of the elder woman is unclear. Using FISH we screened the number of chromosome 21 in preimplanted embryos of 5 elderly women (average age, 38.4 years) to study the feasibility and necessity of screening trisomy 21 in embryos in patients over 35 years old at the in vitro fertilization (IVF) center.  相似文献   

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