基于炔肟成环的5-取代异噁唑-3-羧酸酯类化合物的合成

异噁唑结构普遍存在于药物结构中,同时也在许多天然活性产物结构中存在,而5-取代异噁唑-3-羧酸酯类化合物是异噁唑化合物中研究较为广泛的一类。总结了炔肟成环制备5-取代异噁唑-3-羧酸酯类的合成方法和研究进展,详细归纳和报道各代表性例子,并对其加以对比分析。     

伊索昔康的合成方法研究

研究并合成一种昔康类非甾体抗炎药——4-羟基-2-甲基-N-(5-甲基-3-异噁唑基)-2H-1,2-苯并噻嗪-3-羧酰胺-1,1-二氧化物(伊索昔康).以糖精钠(1)和氯乙酸甲酯为原料,经取代、重排扩环、甲基化反应生成4-羟基-2-甲基-2H-1,2-苯并噻嗪-3-羧酸甲酯1,1-二氧化物(4)中间体,化合物(4)与5-甲基-3-异噁唑胺发生酰胺化反应生成伊索昔康(5).目标产物总收率为64.6％,纯度达100％,其结构由1H-NMR和MS表征.     

基于酮肟成环法的5-取代异唑-3-羧酸酯类化合物合成进展

5-取代异唑-3-羧酸酯类化合物广泛存在于许多药物结构片段中,是药物研发的重要中间体。综述了近年来报道的以酮和盐酸羟胺形成肟而成环这一主要制备方法的研究进展,对代表性化合物的合成进行了详细归纳和总结,并对此类方法的不同物质合成方法的差异、难易等方面加以对比和分析。     

新环3-氧代-5H-5-取代芳基异(噁)唑[3,4-e]并-1,2,3,4-四嗪衍生物的合成

合成了6种3-氨基-5-氧代-4-芳基偶氮异唑衍生物和3-氧代-5-取代芳基异唑[3,4-e]并-1,2,3,4-四嗪衍生物,经元素分析I、R和质谱分析确定了其结构。     

5-取代-1H-1,2,4-三氮唑-3-羧酸的合成及结构表征

以5 氯基 1H 1,2,4 三氮唑 3 羧酸乙酯为原料,经Sandmeyer反应合成了5 取代 1H 1,2,4 三氮唑 3 羧酸乙酯,其中取代基为氯、溴、碘、氰基等。并通过UV,IR,1HNMR和元素分析对所有产物的结构进行了表征。     

取代异噁唑甲酰基脲的合成及其抑菌活性

以5-甲基-3-(取代)苯基-4-异噁唑甲酰胺及取代苯胺为起始原料,经两步反应合成了10种N-取代苯基-5-甲基-3-(取代)苯基-4-异噁唑甲酰基脲新化合物,其结构经1HNMR、IR和元素分析确证。初步测试了目标化合物对番茄灰霉病菌和小麦纹枯病菌的室内抑菌活性,结果表明,部分化合物对番茄灰霉病菌表现出较好的抑菌活性。     

新环3-氧代-5H-5-取代芳基异嗯唑[3，4-e]并-1，2，3，4．四嗪衍生物的合成

合成了6种3-氨基-5-氧代-4-芳基偶氮异噁唑衍生物和3-氧代-5-取代芳基异噁唑[3，4-e]并-1，2，3，4-四嗪衍生物，经元素分析、IR和质谱分析确定了其结构。     

5-取代-1H-1,2,4-三氮唑-3-羧酸的合成及结构表征

以 5- 氨基 1H -1,2 ,4 -三氮唑 3 -羧酸为原料 ,经重氮化反应及Sandmeyer反应得到 5 - 氯、5 -溴、5 -碘、5- 氰基 1H -1,2 ,4 - 三氮唑 3 -羧酸 ,通过UV ,IR ,1HNMR和元素分析对所有产物的结构进行了表征。     

基于1,3-偶极环加成的新型螺[吲唑-异噁唑]衍生物合成及表征

以1-苯基-6,7-二氢-1H-吲唑-4(5H)-酮和取代芳香醛为原料,在碱性条件下缩合得到5-芳亚甲基-1-苯基-6,7-二氢-1H-吲唑-4(5H)-酮,再与腈氧化物进行1,3-偶极环加成得到系列4'-(4-芳基)-3'-(2,6-二氯苯基)-1-苯基-6,7-二氢-4'H-螺[吲唑-5,5'-异噁唑]-4(1H)-酮新化合物,采用NMR、IR、MS以及元素分析表征其结构。     

6-氮杂吲唑-3-羧酸的合成

文章以4-氯-3-硝基吡啶为原料,经取代,脱羧,还原,重氮化环合,水解等六步反应,合成了6-氮杂吲唑-3-羧酸,最终产物及中间体的结构经1H NMR和MS确定。     

Many Drugs of Abuse May Be Acutely Transformed to Dopamine,Norepinephrine and Epinephrine In Vivo

It is well established that a wide range of drugs of abuse acutely boost the signaling of the sympathetic nervous system and the hypothalamic–pituitary–adrenal (HPA) axis, where norepinephrine and epinephrine are major output molecules. This stimulatory effect is accompanied by such symptoms as elevated heart rate and blood pressure, more rapid breathing, increased body temperature and sweating, and pupillary dilation, as well as the intoxicating or euphoric subjective properties of the drug. While many drugs of abuse are thought to achieve their intoxicating effects by modulating the monoaminergic neurotransmitter systems (i.e., serotonin, norepinephrine, dopamine) by binding to these receptors or otherwise affecting their synaptic signaling, this paper puts forth the hypothesis that many of these drugs are actually acutely converted to catecholamines (dopamine, norepinephrine, epinephrine) in vivo, in addition to transformation to their known metabolites. In this manner, a range of stimulants, opioids, and psychedelics (as well as alcohol) may partially achieve their intoxicating properties, as well as side effects, due to this putative transformation to catecholamines. If this hypothesis is correct, it would alter our understanding of the basic biosynthetic pathways for generating these important signaling molecules, while also modifying our view of the neural substrates underlying substance abuse and dependence, including psychological stress-induced relapse. Importantly, there is a direct way to test the overarching hypothesis: administer (either centrally or peripherally) stable isotope versions of these drugs to model organisms such as rodents (or even to humans) and then use liquid chromatography-mass spectrometry to determine if the labeled drug is converted to labeled catecholamines in brain, blood plasma, or urine samples.     

Sapindaceae,cyanolipids, and bugs

Scentless plant bugs (Heteroptera: Rhopalidae) are so named because adults of the Serinethinae have vestigial metathoracic scent glands. Serinethines are seed predators of Sapindales, especially Sapindaceae that produce toxic cyanolipids. In two serinethine species whose ranges extend into the southern United States,Jadera haematoloma andJ. sanguinolenta, sequestration of host cyanolipids as glucosides renders these gregarious, aposematic insects unpalatable to a variety of predators. The blood glucoside profile and cyanogenesis ofJadera varies depending on the cyanolipid chemistry of hosts, and adults and larvae fed golden rain tree seeds (Koelreuteria paniculata) excrete the volatile lactone, 4-methyl-2(5H)-furanone, to which they are attracted.Jadera fed balloon vine seeds (Cardiospermum spp.) do not excrete the attractive lactone. Loss of the usual heteropteran defensive glands in serinethines may have coevolved with host specificity on toxic plants, and the orientation ofJadera to a volatile excretory product could be an adaptive response to save time.Mention of a commercial product does not consititute an endorsement by the USDA.     

Insect antifeedant properties of anthranoids from the genusVismia

Vismiones and ferruginins, representatives of a new class of lypophilic anthranoids from the genusVismia were found to inhibit feeding in larvae of species ofSpodoptera, Heliothis, and inLocusta migratoria.     

2008～2009年世界塑料工业进展

收集了2008年7月～2009年6月世界塑料工业的相关资料,介绍了2008～2009年国外塑料工业的发展情况,提供了世界塑料产量、消费量及全球各类树脂的需求量及产能情况。按通用热塑性树脂(聚乙烯、聚丙烯、聚苯乙烯、聚氯乙烯、ABS树脂)、工程塑料(尼龙、聚碳酸酯、聚甲醛、热塑性聚酯、聚苯醚)、特种工程塑料(聚苯硫醚、液晶聚合物、聚醚醚酮)、通用热固性树脂(酚醛、聚氨酯、环氧树脂、不饱和聚酯树脂)不同品种的顺序,对树脂的产量、消费量、供需状况及合成工艺、产品应用开发、树脂品种的延伸及应用的进一步扩展等技术作了详细介绍。     

ICP-MS法测定地球化学样品中As、Cr、Ge、V等18种微量痕量元素的研究

建立了测定地球化学样品中包括As、Cr、Ge、V等18种微量、痕量元素的ICP-MS方法。地化试样用HF-HNO3混酸分解后,以1 1 HNO3溶解干渣。由于制样不使用盐酸,避免了Cl对As、Cr、Ge、V的质谱干扰。用国家一级地球化学标准物质GBW 07309制备溶液优化仪器工作参数,并用于校准。方法测定限(6s)为:0.007~6.4μg/g,精密度(RSD%,n=12)为:29%~9.4%,经过国家一级地球化学标准物质的分析验证,结果与标准值吻合。方法已应用于国土资源调查的试样分析。