对丙氧基苦杏仁酸的合成

本文以苯丙醚为原料，经酰化、溴化和水解反应合成了苯并二呋喃酮类染料分散红356的重要中间体一对丙氧基苦杏仁酸。探讨优化了酰化反应和溴化反应的反应条件，这三步反应的收率分别80．9％，78．0％和84．7％。     

荧光增白剂CBS-127合成工艺研究

以联苯二氯苄、亚磷酸三甲酯、邻甲氧基苯甲醛为原料经膦酰化、缩合反应制备荧光增白剂CBS-127，最佳工艺条件：膦酰化反应物料m(联苯二氯苄)：m(亚磷酸三甲酯)为1：1．24，加料温度140℃，甲醇用量1．50mL，反应时间2h；缩合反应温度50℃，物料配比m(膦酰化反应产物)：m(邻甲基苯甲醛)为1：0．85。该条件下反应总收率80％以上，产品增白强度(相对于标准品)为102％。     

2—甲氧基—5—氨基苯—β—羟乙基砜合成研究

本文以对氨基苯甲醚为原料．经酰化、氯磺化、还原、缩合、水解等反应，制取了２－甲氧基－５－氨基苯－β－羟乙基砜，总收率６７．４％。     

活性大红3G的合成研究

以2,4-二氨基苯磺酸钠、2,3-二溴丙酰氯和1酸为原料,经酰化、重氮化、偶合和盐析制得活性大红3G。重点研究了两步酰化过程。通过实验得到了较完整的反应条件：酰化温度0～15℃,pH控制在5—7．5,2,3．二溴丙酰氯与2,4-二氨基苯磺酸钠的投料比是1．05：1;2,3-二溴丙酰氯与γ酸的投料比也是1．05：1,酰化收率达90％以上。     

2—甲氧基—5—氨基苯—β—羟乙基砜合成研究

本文以对氨基苯甲醚为原料，经酰化、氯磺化、还原、缩合、水解等反应，制取了２－甲氧基－５－氨基苯－β－羟乙基砜，总收率６７．４％。     

C．I．酸性蓝350染料合成工艺研究

以2，4-二氨基甲苯和1-氨基-2-磺酸基-4-溴-9，10-蒽醌为原料，经酰化、缩合、水解、磺酰化后盐析得C．I酸性蓝350染料。重点研究了关键步骤水解反应过程。通过实验得到了较佳的反应条件：酸性条件下，缩合物与乙醇投料比1：200，时间19～21h，水解反应收率达93％。     

黑豆皮花色苷的酶法酰化制备及其稳定性分析

以黑豆皮花色苷矢车菊素-3-O-葡萄糖苷（cyanidin-3-O-glucoside，C3G）为原料，采用月桂酸为酰基供体，经酶法酰化制备具有亲脂性能的花色苷脂肪酸酰化产物。分别以黑豆皮粗提物（C3G含量35.8%）、纯化C3G样品（纯度>80%）、C3G标准品（纯度>98%）为底物进行酰化，通过改进反应溶剂体系，实现了黑豆皮粗提物中花色苷的高效酰化，酰化率达66.59%，产率达到C3G标准品酰化的75%，但工艺更为简单，底物无需纯化；酰化产物矢车菊素-3-O-葡萄糖苷月桂酸酰化物（cyanidin-3-O-glucoside-lauric acid，C3G-La）经液液萃取，纯度可达82.39%；经进一步正相硅胶分离纯化后，产物纯度达97.58%。稳定性试验发现，在pH为中性和酸性环境中，C3G-La的稳定性优于C3G，但二者在碱性和光照条件下稳定性均较差。     

米曲霉氨基酰化酶拆分DL茶氨酸

DL-茶氨酸经乙酰化可生成N-乙酰-DL-茶氨酸，然后利用米曲霉氨基酰化酶拆分N-乙酰-DL-茶氨酸可以获得L-茶氨酸。本文对氨基酰化酶酶促反应也进行了初步研究，考察了反应温度、反应时间、pH值和底物浓度等因素对酶促反应的影响。实验表明，转化温度40℃、转化时间30h、pH为7．0和底物浓度0．2mol／L时，目的产物L-茶氨酸的产率最高。     

乙氧苯酯的合成工艺改进

以对氨基水杨酸为原料，经酯化、酰化和烃化反应得乙氧苯酯，总收率为８７．４％。讨论了投料比、反应温度和反应时间对收率的影响，并改进了合成工艺。     

间乙酰胺基－N－乙基－N－苄基苯胺合成工艺研究

研究了由间苯二胺经单氨基酰化、氯化苄苄基化及溴乙烷乙基化合成间乙酰胺基－Ｎ－乙基－Ｎ－苄基苯胺的工艺，总收率达７１．２４％。     

对乙基苯乙烯的合成研究(Ⅰ)——乙苯的乙酰化反应

通过乙苯的乙酰化反应、还原反应、脱水反应可以制备对乙基苯乙烯 ,其中乙酰化反应是重要步骤。在本工作中 ,采用气相色谱对乙酰化反应过程跟踪测试 ,研究反应条件对收率和选择性的影响 ,优化反应条件。同时 ,以红外光谱、核磁共振等手段对产物进行了表征     

Exploring the Minimal RNA Substrate of Flexizymes

Flexizymes are tRNA acylation ribozymes that have been successfully used to facilitate genetic code reprogramming. They are capable of charging acid substrates onto various tRNAs and tRNA analogues. However, their minimal RNA substrate has not been investigated. Here we have designed fluorescently labeled short RNAs corresponding to the four, three, and two bases (4bRNA, 3bRNA, 2bRNA) at the tRNA 3′-end and explored the minimal RNA substrate of flexizymes, dFx and eFx. 3bRNA was the observed minimal RNA substrate of the flexizymes, but the efficiency of acylation of this short RNA was two to three times lower than that of 4bRNA. The efficiency of acylation of 4bRNA was comparable with that of the microhelix, a 22-base RNA conventionally used as a tRNA analogue for analyzing acylation efficiency. We also compared the efficiencies of acylation of the microhelix and 4bRNA with various acid substrates. Thanks to the short length of 4bRNA, its acyl-4bRNA products exhibited larger mobility shifts in gel electrophoresis than those exhibited by acyl-microhelix products with every substrate tested. This indicated that 4bRNA was an ideal RNA substrate for analyzing the efficiency of acylation by flexizymes.     

Role of mineral matter in the chemical reactivity of coal

Previous work showed that the solvent extraction yield of coal increased as a result of chemical reactions such as formylation, reductive acylation, acylation, amidomethylation, alkylation, reduction and depolymerization. In the work described in this Paper, dmmf coal obtained after demineralization with mixed HF-HCI acids was used for solvolytic extraction studies after depolymerization, alkylation, acylation, amidomethylation, reductive acylation and reduction reactions. In comparison with the original coal, mineral matter free coal showed less increase in extractability as a result of these reactions indicating that mineral matter present in the original coal was acting as a promoter for these reactions.     

硝基苯加氢一锅法合成对乙酰氨基苯酚

针对目前工业上现有对乙酰氨基苯酚(APAP)合成工艺存在的问题,探索了乙酸和锌盐混合溶液中以硝基苯为原料一锅法直接合成APAP新工艺,对对氨基苯酚(PAP)的酰化反应以及酰化与加氢反应的耦合过程进行了研究和分析。结果表明:乙酸和锌盐在促进苯基羟胺重排生成PAP上具有明显的协同促进作用,可明显提高加氢反应中生成PAP的选择性,选择性最高达到了76.8%。加氢反应过程中,硫酸锌对乙酸和PAP的酰化反应具有明显的抑制作用,而乙酸锌的影响则明显要小。乙酸锌浓度为170 mmol/L时,乙酸对PAP酰化反应转化率可以达到50%以上。采用加氢反应结束后降温再利用乙酸酐酰化的方法可使生成的PAP完全转化为APAP,APAP最高收率超过70%。     

聚醚多元醇羟值测定方法探讨

对测定聚醚多元醇羟值的酰化方法进行探讨,提出了操作简便,快速适用的咪唑催化的乙酸酐-丙酮体系催化酰化法。该催化酰化反应水浴加热至（50±1）℃,反应30 min。与国标法相比,该催化酰化法避免使用有毒的吡啶试剂,且完成一次测定耗时可从国标方法的2 h缩短至30 min。改进后的方法具有简单、快速、准确等优点。     

酶促吉西他滨乙酰化反应的研究

探讨了八种不同来源水解酶催化吉西他滨乙酰化反应的催化活性,结果发现,有四种脂肪酶能够催化该酰化反应,且它们的产物只有一种,其中脂肪酶Novozyme435的催化活性最高。此外,通过13C-NMR和MS等技术手段对酶促反应产物的结构进行鉴定,发现它们以催化吉西他滨5’-羟基酰化反应为主,且反应选择性均高于99%。     

酰化反应合成N-(2-溴-4-甲氧基苯基)丙烯酰胺的研究

研究了2-溴-4-甲氧基苯胺与丙烯酰氯发生酰化反应合成了N-(2-溴-4-甲氧基苯基)丙烯酰胺的方法。以95.7%的收率得到N-(2-溴-4-甲氧基苯基)丙烯酰胺。探讨了反应物物质的量比、反应时间、反应温度和碱的添加对酰化反应的影响。该方法原料易得,反应条件易于控制,收率高,对环境友好。     

Effect of high fat/high erucic acid diet on phosphatidate synthesis and phosphatidate phosphatase in the subcellular fractions of rat heart and liver

Rats of weaning age were fed for a period of 1,3 or 6 weeks either a control diet (laboratory stock diet) or a semisynthetic diet containing 20% by weight of either mustard seed oil (1/3 of the total fatty acids were comprised of erucic acid) or corn oil (2/3 of the total fatty acids consisted of linoleic acid). Mitochondrial and microsomal fractions were isolated from the hearts and livers of these rats, and the rate of acylation ofsn-[U-¹⁴C] glycerol 3-phosphate (P) was examined using palmitoyl-CoA or erucoyl-CoA as the acyl donor. In addition, activities of phosphatidate phosphatase of the mitochondrial, microsomal and soluble fractions were assayed. Studies on the acylation of glycerol 3-P with palmitoyl-CoA demonstrated that feeding of the high fat/high erucic acid diet for 1,3 or 6 weeks significantly increased the rate of formation of monoacylglycerol 3-P by the cardiac subcellular fractions as compared to the control. The rate of formation of diacylglycerol 3-P also increased but to a lesser degree. Feeding the high fat/high linoleic acid diet tended to increase acylation of glycerol 3-P by cardiac subcellular fractions. However, neither high fat diet influenced acyltransferase activities of the hepatic subcellular fractions or phosphatase activities of the cardiac and hepatic fractions. Studies on the acylation of glycerol 3-P with erucoyl-CoA demonstrated that the rate of acylation was ca. 1/10 that measured using palmitoyl-CoA in all experiments; in particular, the formation of diacylglycerol 3-P was extremely slow, suggesting that erucoyl-CoA is an unsuitable substrate for the position-2 of the monoacylglycerol 3-P. The rate of acylation by the cardiac and hepatic subcellular fractions was not influenced by the feeding of the high-fat diets. The rate of glycerol 3-P acylation by both cardiac and hepatic mitochondrial fraction was ca. 2/3 of the rate of acylation by the respective microsomal fraction. In addition, the ratio of monoacyl-to diacylglycerol 3-P synthesized by the mitochondrial fraction was smaller than that by the microsomal fraction. These results suggest that acylation of glycerol 3-P by the mitochondrial cannot be attributed to the action of the contaminating microsomal enzymes.     

4-(3,4-二氯苯基)-3,4-二氢-1(2H)-萘酮的合成

邻二氯苯和丁二酸酐经付-克酰化制得,再经还原、付-克酰化和闭环等反应得到抗抑郁剂舍曲林的中间体4-(3,4-二氯苯基)-3,4-二氢-1(2H)-萘酮,总收率50%。第1步反应n(AlCl3):n(丁二酸酐)=2.2:1较为适宜。     

6-甲氧基-2-丙酰萘生产工艺改进

以 β 萘酚为原料 ,以 1,2 二氯乙烷及硝基甲烷代替剧毒物质硝基苯作为丙酰化反应中的溶剂 ,经甲醇、硫酸甲基化 ,丙酰氯、无水三氯化铝丙酰化制备 6 甲氧基 2 丙酰萘 ,总收率达73 8%。