含氮杂环的芳甲酰基硫脲的合成及其生物活性

合成了7个新的含安替比林基的芳甲酰基硫脲类化合物（5a-5g）,其结构经^1H NMR,IR和元素分析确证。对5进行的室内生物活性测试结果表明,部分5对某些真菌具有较高的抑菌率,其中5c和5f对黄瓜灰霉的抑菌率分别达到96．23％和94．34％。     

二茂铁及其胺甲基类取代衍生物的紫外光解自由基的研究

本文用自旋捕捉-ESR技术研究了二茂戊铁、环二烯和胺甲基类取代二茂铁的紫外光解过程中的活泼自由基。结果表明,二茂铁光解初级过程中生成的自由基为(C_5H_5Fe)·和C_5H_5·,其衍生物光解则生成(C_5H_5Fe)·和RC_5H_4·,而(C_5H_5Fe)·还可以进一步分解给出C_5H_5和Fe。     

稀土元素对腺嘌呤及鸟嘌呤单核苷酸的水解断裂作用

本文研究稀土元素对5'-腺嘌呤核苷酸(5'-AMP)和5'-鸟嘌呤核苷酸(5'-GMP)的水解断裂作用。空气中CeCl~3在pH 9,37℃能有效地水解断裂5'-AMP及5'-GMP,而其它三价稀土对5'-AMP和5'-GMP的水解断裂作用很小, 铈对5'-AMP的水解断裂速度大于5'-GMP。紫外吸收光谱实验结果表明反应体系中Ce(Ⅲ)部分被氧化成Ce(Ⅳ), Ce(Ⅳ)的氢氧簇合物是使5'-AMP和5'-GMP水解的活性组分。     

一茂二元羧酸镱的合成

本文报道了五个新的一茂二元羧酸镱的合成:o-C_6H_4(COO)_2YbC_5H_5(1),(CH_2COO)_2YbC_5H_5(2),(CHCOO)_2YbC_5H_5(3),CH_3(COO)_2YbC_5H_5(4),(COO)_2YbC_5H_5(5),这些络合物均经元素分析和红外光谱鉴定。可能由于这些络合物具有螯合环的结构,所以它们在空气中的隐定性较强。     

烟草中糖的毛细管区带电泳分离

 采用高效毛细管电泳 紫外吸收法 (HPCE UV) ,以对氨基苄腈为衍生试剂 ,通过改进缓冲溶液添加剂 ,对烟草中 5种糖的衍生物进行了分离。该法使用 pH 10 5 ,5 0mmol/L硼砂缓冲液 ,其中添加剂含量为甲醇 5 % (体积分数 ,下同 )、乙腈 5 %、乙二醇 2 5 %、异丙醇 2 5 %和十二烷基硫酸钠 (SDS) 1mmol/L。测定波长为 2 85nm。     

5-硝基-2H-四唑的合成、反应性及产物晶体结构的研究

5-氨基四唑(1)经过重氮化反应得到5-硝基四唑(5),5与甲醛反应得到2-羟甲基-5-硝基四唑(6),6与HCl或HBr反应分别得到5-5氯代四唑(7)和5-溴代四唑(8),采用MS,IR,1H NMR,13C NMR等技术对这些化合物进行了表征.用X射线单晶衍射法测定了化合物5-硝基四唑钠(4),5和6的晶体结构.化合物4属于三斜晶系,P-1空间群;化合物5和6均属于单斜晶系,P21空间群,化合物6的晶胞参数a=0.66131(18)nm,b=0.54905(15)nm,c=0.7566(2)nm,Z=2,V=0.27470(13)nm3,Dc=1.754g/cm3,F(000)=128,μ=0.160mm-1.     

新型取代苯乙醇葡萄糖氧苷的合成及其抗缺氧活性

以取代苯甲醛为原料,经Wittig反应、水解反应和NaBH₄还原反应制得5个取代苯乙醇衍生物（4a~4e）;以4a~4e和其他芳乙醇（4f~4r）为原料,依次与全乙酰化溴代葡萄糖经Koenigs-Knorr偶联和MeONa/MeOH脱除乙酰保护基,合成了18个取代苯乙醇葡萄糖氧苷类似物（5a~5r,其中5b~5r为新化合物）,其结构经¹H NMR和HR-MS（ESI）表征。采用MTT法研究了5a~5r对缺氧损伤的内皮细胞（EA.hy926）代谢活力的影响。结果表明：5e, 5g, 5m, 5p, 5q和5r对EA.hy926的保护作用优于红景天苷。     

稀土元素对腺嘌呤及鸟嘌呤单核苷酸的水解断裂作用

本文研究稀土元素对5’-腺嘌呤核苷酸(5’-AMP)和5’-鸟嘌呤核苷酸(5’-GMP)的水解断裂作用.空气中CeCl_3在pH9,37℃能有效地水解断裂5’-AMP及5’-GMP,而其它三价稀土对5’-AMP和5’-GMP的水解断裂作用很小,铈对5’-AMP的水解断裂速度大于5’-GMP.紫外吸收光谱实验结果表明反应体系中Ce(Ⅲ)部分被氧化成Ce(Ⅳ),Ce(Ⅳ)的氢氧簇合物是使5’-AMP和5’-GMP水解的活性组分.     

苯丙烯类葡萄糖氧苷的合成及其抗缺氧活性

以取代苯甲醛(1a~1t)为原料,通过Knoevenagel缩合、酯化和LiAlH₄还原等反应制得苯丙烯醇衍生物(3a~3t);以取代肉桂醛(1u~1x)为原料,经NaBH₄还原制得苯丙烯醇衍生物(3u~3x); 3a~3x与全乙酰化溴代葡萄糖经Koenigs-Knorr偶联反应及MeONa/MeOH体系脱除乙酰保护基反应,合成了24个苯丙烯类葡萄糖氧苷(5a~5x),其中5c,5f ~ 5x为新化合物,其结构经¹H NMR和ESI-MS表征。采用MTT法测定了5对缺氧损伤的内皮细胞(EA.hy926)的抗缺氧活性。实验结果表明： 5b, 5e, 5g, 5p, 5q, 5s, 5t和5y对EA.hy926的抗缺氧活性均高于经景天苷。     

新型吡唑啉衍生物的合成及其对Fe(Ⅲ)的选择性识别

以芳酮和芳醛为原料,在Na OH/Et OH存在下经缩合反应制得中间体芳烯酮(3);3与肼经环合反应合成了5个新型的含荧光基团的吡唑啉衍生物(5a~5e),其结构经1H NMR,13C NMR和IR表征。并利用UVVis和FL研究了5a~5e对金属离子的选择识别性能。结果表明,5a~5e对Fe(Ⅲ)有较好的选择性识别。     

The Synthesis of 1-Aryl-5-Fluorouracil

5-Fluorouracil (5-Fu,1)1 is an important antitumor drug. Some derivatives2,3 have shown better therapeutic efficacy than 5-Fu. In order to find much more better antitumor drugs of its derivatives, several attempts have been made and many different types of its derivatives have been prepared at N1, N3 position4~7. Moreover, several different ways have been used for alkylation of 5-Fu7~10. However, up to now, the arylation of 5-Fu at N1 or N3 position hasn't been reported, and the compound o…     

含5-氟尿嘧啶的氨基酸衍生物的合成及其抗肿瘤活性研究

5-氟尿嘧啶乙酸对硝基苯酯和5-氟尿嘧啶丙酸对硝基苯酯与一系列氨基酸反应,制备了12个新的含5-氟尿嘧啶的氨基酸衍生物,并确定了化合物的结构。初步动物试验表明某些化合物有一定的抗肿瘤活性。     

The Synthesis of 6-Alkyl-5-Fluorouracil Derivatives

As an antitumor drug, because of its low efficacy and high toxicity, several modifications have been made on 5-fluorouracil (5-Fu). Some compounds have been found to be highly efficient and much less toxic for the treatment of various solid tumors1~4. Among them, deoxyfluridine (Furtulon) has been used clinically for several years. In our previous work, we have prepared several substituted derivatives of 5-Fu and the primary result shows that some of them have certain antitumor activity5,6. …     

氟脲嘧啶自旋标记衍生物的合成与抗肿瘤活性（Ⅲ）

合成了９个新的５－氟脲嘧啶自旋标记衍生物２、５ａ－ｃ和７ａ－ｃ，经元素分析、ＩＲ、ＵＶ、ＭＳ和ＥＳＲ确定了其组成和结构，对化合物２和５ａ－ｃ进行了抗小艾氏腹水肉瘤Ｓ１８０的体内筛选，初步试验结果表明：化合物５ｃ对两种瘤株均显示较强的抑制作用，其抗肿瘤活性与５－氟脲嘧啶相似，而５ｃ（ＬＤ５０＝９４４．８ｍｇ／ｋｇ）的急性毒性比５－氟脲嘧啶（ＬＤ５０＝１１７．２ｍｇ／ｋｇ）降低约８倍。     

Synthesis and antitumor activity of N^1-acetylamino-（5-alkyl/aryl-1,3,4-thiadiazole-2-yl）-5-fluorouracil derivatives

A new series of N^1-acetylamino-（5-alkyl/aryl- 1,3,4-thiadiazole-2-yl）-5-fluorouracil derivatives were designed and synthesized. These compounds have not been reported in literature, and their structure chemical were confirmed by IR, ^1H NMR and MS （HRMS）. The results of antitumor inhibitory activity test showed that some compounds possess more potent antitumor inhibitory activity than 5-fluorouracil.     

Synthesis and antitumor activity of N1-acetylamino-(5-alkyl/aryl-1,3,4-thiadiazole-2-y1)-5-fluorouracil derivatives

A new series of N1-acetylamino-(5-alkyl/aryl- 1,3,4-thiadiazole-2-y1)-5-fluorouracil derivatives were designed and synthesized.These compounds have not been reported in literature,and their structure chemical were confirmed by IR,1H NMR and MS (HRMS).The results of antitumor inhibitory activity test showed that some compounds possess more potent antitumor inhibitory activity than 5-fluorouracil.     

Synthesis of 1- and 3-arylcarbonyl derivatives of 5-fluorouracil

4′-Substituted 1-arylcarbonyl-5-fluorouracil derivatives were synthesized from the reaction of the potassium salt of 5-fluorouracil with one equivalent of aryl acid chloride in acetonitrile. 4′-Substituted 3-arylcar-bonyl-5-fluorouracil derivatives were synthesized from the reaction of 5-fluorouracil with 3 equivalents of the aryl acid chloride in pyridine and the subsequent hydrolysis of the 1,3-diarylcarbonyl-5-fluorouracil derivatives in situ with a small amount of water. If a large amount of water were used in the second step, the 1,3-diarylcarbonyl-5-fluorouracil precipitated before it hydrolyzed. The melting behaviors of both the 1-arylcarbonyl-5-fluorouracil and 3-arylcarbonyl-5-fluorouracil series suggested that thermal decomposition or rearrangement occurred on heating. The position of the C⁶-H absorption in the ¹H nmr spectra of 1-arylcarbonyl-5-fluorouracils was 0.14 to 0.23 ppm farther downfield than that of the corresponding 3-arylcarbonyl-5-fluorouracils while that of the 1,3-diarylcarbonyl-5-fluorouracils was even farther downfield. The Rf values of 1-arylcarbonyl-5-fluorouracils were significantly greater (0.23 to 0.41) than those of the corresponding 3-arylcarbonyl-5-fluorouracils, while that of 1,3-diarylcarbonyl-5-fluorouracil was slightly greater than that of 1-arylcarbonyl-5-fluorouracils.     

含氨基酸席夫碱的5-氟尿嘧啶衍生物的合成及其抗肿瘤活性

以N 1-(2-四氢呋喃烷基)-5-氟尿嘧啶为原料, 与1,4-二溴丁烷反应, 得到N¹-(2-四氢呋喃烷基)-N³-(4-溴丁基)-5-氟尿嘧啶(2), 最后与氨基酸席夫碱的钾盐缩合, 得到13个新的目标化合物3. 其结构经IR, ¹H NMR, MS和元素分析确证. 初步的体外抗肿瘤试验结果表明, 目标化合物具有一定的抗肿瘤活性.     

New acetenyl acyclic nucleosides synthesis of 1-(propargyloxymethyl) derivatives of uracil

Alkylation of trimethylsilyl derivatives of uracil, thymine, 5-fluorouracil, and 6-methyluracil with propargyloxymethyl chloride afforded the corresponding 1-(propargyloxymethyl) derivatives, new unsaturated acyclic nucleosides having an end carbon-carbon triple bond.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 797–799, June, 1993.     

Synthesis of a New Series of Bone Affinity Compounds

As known that tetracycline possesses bone affinity1, which can be used as carrier of bone-targeting drugs. Chrysophanol is one of the anthraquinone components isolated from Rheum palmatum L., its structure is similar to tetracycline. The bone affinity of …