Indoxyl derivatives of drug metabolites

Summary Indoxyl derivatives were detected as minor products among the urinary metabolites of two trial drugs, a benzodiazepine (GP 55 129) and a benzophenone (CGP 11 952). Their structures were elucidated by NMR and mass spectroscopy. Presumably, metabolites containing potential aldehyde functions react spontaneously with endogenous indoxyl. Such derivatives have not hitherto been encountered in drug metabolism.     

Selectivity determinants of the aldose and aldehyde reductase inhibitor-binding sites

Aldose reductase and aldehyde reductase belong to the aldo-keto reductase superfamily of enzymes whose members are responsible for a wide variety of biological functions. Aldose reductase has been identified as the first enzyme involved in the polyol pathway of glucose metabolism which converts glucose into sorbitol. Glucose over-utilization through the polyol pathway has been linked to tissue-based pathologies associated with diabetes complications, which make the development of a potent aldose reductase inhibitor an obvious and attractive strategy to prevent or delay the onset and progression of the complications. Structural studies of aldose reductase and the homologous aldehyde reductase in complex with inhibitor were carried out to explain the difference in the potency of enzyme inhibition. The aim of this review is to provide a comprehensive summary of previous studies to aid the development of aldose reductase inhibitors that may have less toxicity problems than the currently available ones. Received 4 December 2006; received after revision 12 February 2007; accepted 20 April 2007     

乙酸乙酯生产工艺现状及发展趋势

介绍了国内外乙酸乙酯的生产工艺现状和发展趋势，并对酯化法和乙醛缩合法的工艺条件，技术经济情况进行了对比。     

微波辐射下合成5-亚苄基绕丹宁乙酸

利用微波辐射催化芳香醛与绕丹宁乙酸的缩合反应,合成了10个5-亚苄基绕丹宁乙酸衍生物,反应时间8~20 min,产率较好,操作简便.     

由α-蒎烯合成一些昆虫保幼激素类似物

由α-蒎烯得到的蒎酮醛、龙脑烯醛、2,2-二甲基-3-乙基环丁基乙醛为起始原料,经Wittig或Wittig-Horner反应合成了昆虫保幼激素类似物4-(2,2-二甲基-3-乙基环丁基)-丁-2-烯酸乙酯(Ⅰ),6-(2,2-二甲基-3-乙基环丁基)-已-2,4-二烯酸乙酯(Ⅱ),6-(2,2-二甲基-3-乙基环丁基)-已-2,4-二烯酸甲酯(Ⅲ),6-(2,2-二甲基-3-乙酰基环丁基)-已-2,4-二烯酸甲酯(Ⅳ),6-(2,2,3-三甲基-环戊-3-烯基)-已-2,4-二烯酸甲酯(Ⅴ),3-甲基-8-(2,2-二甲基-3-乙基环丁基)-辛-2,6-二烯酸乙酯(ⅤⅢ)。它们的结构经红外光谱、1~H核磁共振和元素分析鉴定。     

微波辐射下9—芳基—3,3,6,6—四甲基—1，8—二氧代—1，2，3，4，5，6，7，8，9，10—十氢吖啶的合成

对氯苯甲醛（或3，4-二甲氧基苯甲醛），5，5-二甲基-1，3-环己二酮，醋酸铵为原料在无溶济条件下经微波辐射得9-对氯苯基-3，3，6，6-四甲基-1，8-二氧代-1，2，3，4，5，6，7，8，9，10-十氢吖啶，结构通过红外光谱、核磁共振谱，元素分析确定。     

脂肪醇氧化制取脂肪醛

利用混合脂肪醇减压蒸馏获得的 C_8、C_9、C_(10)、C_(11)醇,在电解银催化剂存在下,氧化制取相应脂肪醛。研究了反应条件对转化率、选择性和收率的影响。转化率、选择性达到了90%以上。     

酚醛树脂碳化产物作为锂离子电池碳电极材料(Ⅱ)──锂离子电池充放电性能测试

测试分析了酚醛树脂碳化产物组装的锂离子充放电性能．实验结果表明，树脂碳化 产物作为锂离子电池碳电极材料时，其碳化处理温度有一个最佳温度范围，酚醛树脂碳化产物 的最佳温度在７００℃左右；树脂碳化产物的比表面积是影响电池充放电性能的重要因素，碳化 产物的比表面积越大，电池的充放电量就越高，电池充放电量与充放电电流密度成反比．     

聚醋酸乙烯缩醛乳液实验条件探讨

将聚乙烯醇（ＰＶＡ）溶于水中，加入非离子型表面活性剂，以（ＮＨ４）２Ｓ２Ｏ８为引发剂，先进行醋酸乙烯（ＶＡＣ）的乳液聚合。然后在一定条件下，加入甲醛进行缩聚反应，最后加入填料和增塑剂，得到产品。本实验条件较之聚醋酸乙烯实验条件易控制，产品粘接能力强，在工业生产中具有实用价值。本文主要讨论实验条件的选择     

酚醛树脂对NR硫化胶性能的影响

详细讨论了酚醛树脂／六亚甲基四胺用量对天然橡胶硫化胶物理机械性能及动态力学性能的影响，用电子扫描电镜（ＳＥＭ）研究了硫化胶磨耗表面状态。结果表明，随酚醛树脂用量增加，硫化胶硬度，１００％定伸应力，动态弹性模量增加，而扯断伸长率，撕裂强度及动态力学损耗（ｔａｎδ）下降。当酚醛树脂用量为５份左右时，拉伸强度，３００％定伸应力，耐磨性及耐老化性能最优，ＳＥＭ照片上磨纹最细。