2—氨基—2—噻唑啉—4—羧酸合成工艺研究

DL—2—氨基—△2—噻唑啉—4—羧酸外消旋体（DL—ATC）是生物合成法制备L-半胱氨酸的前体,目前国内尚未实现工业化生产。后者又是广泛用于医药、化妆品和食品等领域的重要生物化学制品,市场需求量相当大。本论文阐述了由丙烯酸甲酯出发,经过氯化、脱氯化氢,加成,环合等步骤制备DL—2—氨基—△2—噻唑啉—4—羧酸（DL—...     

2—甲基—1—丁烯异构为2—甲基—2—丁烯的研究

异戊烯是抽余碳五的一种馏分，主要由两种同分异构体2—甲基—2—丁烯(2MB2)和2—甲基—1—丁烯(2MB1)组成，其中，2—甲基—2—丁烯含量越高，应用价值越高。本研究提供了一种提高异戊烯中2—甲基—2—丁烯含量的方法，即在催化剂作用下，在一定的温度、压力和空速下，以液相形式将2—甲基—1—丁烯异构为2—甲基—2—丁烯。最佳反应条件为：反应温度25—55℃，反应空速5—20hr^-1，反应压力0．6—0．9MPa。在此条件下，异戊烯中的2—甲基—2—丁烯与2—甲基—1—丁烯的比例由原料中的1—4：1提高到10—13：1。     

测癌试剂—γ—1—谷氨酰—1—萘胺的工艺路线与应用

<正> 测癌试剂—γ—l—谷氨酰—l—萘胺对于测定肝胆系统癌症等疾病具有一定的成效。它的工艺路线是由谷氨酸和邻苯二甲酸酐反应后,再与甲萘胺缩合而成。它用于测定癌症的原理简介如下:正常人血清γ—谷氨酰转肽酶的活力很     

2—氰基—4—硝基—6—溴苯胺的合成

标题化合物是合成偶氮分散染料和杂环化合物的重要中间体。本文介绍了由2—氰基4—硝基苯胺(本文简称—氰直接溴化合成法:采用甲醇做溶剂—氰:溴=1:1.2,反应时间1.5小时,收率达90～94％,产品纯度>97％。     

3—氯—4—氟—苯胺的合成

3—氯—4—氟—苯胺(ⅩⅩⅣ)是全合成新型、广谱和高效第三代抗菌素氟哌喹酮酸(Norfloxacin)的重要起始原料合成化合物ⅩⅩⅣ可由芳香族含氮衍生物、如兼含氯者则更佳。笔者收集六个(Ⅰ—Ⅵ)比较普通的芳香族含氮化合物,可作为起始原     

4—氨基—2,6—二甲氧基嘧啶的合成

前言4—氨基—2,6—二甲氧基嘧啶(4—amino—2,6—dimethoxypyrimidine)是一个药物中间体,可用于合成长效磺胺药:2,6—二甲氧基—4—(对氨基苯磺酰胺嘧啶。该药毒性很低,而对上呼吸道和尿道方面的感染特别有效,对肾脏的刺激极为轻微,在血液中的浓度可以维持较长的时     

5，7—二甲基—N—芳基—1，2，4—三唑[1，5—α]嘧啶—2—磺酰胺的合成

以5—氨基—3—巯基—1，2，4—三唑为原料，经氧氯化后分别与6个芳胺反应，得到5氨基—N—芳基1，2，4—三唑—3—磺酰胺，继而和乙酰丙酮于乙酸中环合，制得6个取代的1，2，4—三唑[1，5—α]嘧啶—2—磺酰胺衍生物，同时讨论了胺解反应和环合反应的影响因素。所有目标产物的结构均经IR和^1H NMR谱验证。     

新型2—烷氧基—3—芳基—5—苯基亚甲基—4H—咪唑啉—4—酮衍生物的合成与杀菌活性研究（Ⅱ）

研究了应用烯基膦亚胺与芳基异氰酸酯、醇的串联aza-Wittig反应合成2—烷氧基—3芳基—5—苯基亚甲基—4H—咪唑啉—4—酮衍生物的新方法。探讨了反应进行的条件和产物的波谱性质，提出了可能的环化反应机理。生成的环化产物结构经元素分析、IR、^1HNMR和MS确证。对这些新型杂环化合物的杀菌活性测试结果表明，部分化合物表现出较好的抑菌活性。     

非水滴定法测定2—氨基—4—甲氧基—6—甲基—1,3,5三嗪的含量

本文介绍了以冰乙酸为溶剂,高氯酸的冰乙酸溶液为滴定试剂,以甲基紫为指示剂,测定2—氨基—4—甲氧基—6—甲基—1,3,5—三嗪百分含量的方法。此法简便快速,准确度高,重现性好,可用于指导工业生产。     

致密Bi—Sr—Ca—Cu—O超导体材料的研制

自发现Y—Ba—Cu—O超导体以来,又发现了零电阻温度为110K的Bi—Sr—Ca—Cu—O系(简称BSCCO,以下同)超导体材料和零电阻温度为120K的Tl—Ba—Ca—Cu—O系超导材料,其中BSCCO系超导材料因不含有毒元素及稀土元素而更受人注意。但是这类材料有几个致命的弱点,其中之一是高温相极不稳定,这种高温相既难形成,又很容易转变为低温相,因此较难获得具有单一高温相组成的BSCCO体材料;其次是BSCCO系体材     

Hepatic metabolism of 1-14C octanoic and 1-14C margaric acids

The hepatic metabolism of 1-¹⁴C margaric acid, a 17 carbon long chain saturated fatty acid which is present in the liver in trace amounts, was compared with 1-¹⁴C octanoic acid and 1-¹⁴C palmitic acid to determine if the enhanced oxidation of medium chain fatty acids to CO₂ was dependent on fatty acid chain length or the endogenous pool size of the fatty acid substrate. Despite the fact that endogenous margarate is present in trace amounts, there was no significant difference in the oxidation of margarate and palmitate to CO₂, while the oxidation of octanoate to CO₂ was significantly more rapid. Both margarate and palmitate were more readily incorporated into lipid soluble products in contrast to the low rate of incorporation of octanoate. However, margarate was less readily incorporated into triglyceride, phospholipid and monoglyceride than palmitate. These studies suggest that the chain length rather than hepatic content of the fatty acid determines whether the carboxyl group of equimolar amounts of a 1-¹⁴C-carboxyl labeled fatty acid will be preferentially oxidized to CO₂ or incorporated into tissue lipid in the liver.     

脂肪醇聚氧乙烯醚硫酸钠盐的研制

用氯磺酸作硫酸化试剂，与脂肪醇聚氧乙烯醚（AE0－6）反应，制备脂肪醇聚氯乙烯醚硫酸钠盐（AES），讨论了AES制备条件。     

Processing for industrial fatty acids - I

Palm kernel and coconut oils are particularly important to the fatty acid industry because they are the major sources of lauric acid. This paper describes the processes used to convert these oils to their fatty acids. These in turn may be fractionated into saturated/unsaturated acids and to specific chain lengths by winterization, panning and pressing, fractional distillation, solvent crystallization and hydrophilization methods. The products are important raw materials for the soap, detergent and oleochemical industries. Emery Industries     

Inhibition of fatty acid synthesis in isolated adipocytes by 5-(tetradecyloxy)-2-furoic acid

The compound 5-(tetradecyloxy)-2-furoic acid (TOFA), a hypolipidemic agent, inhibits fatty acid synthesis, lactate and pyruvate accumulation and CO₂ release in isolated at adipocytes. TOFA stimulates the accumulation of citrate. ATP levels are not lowered by TOFA. In comparison with the natural fatty acid, oleate, TOFA exhibited a much greater inhibitory effect on lipogenesis. TOFyl-CoA formation within intact adipocytes was demonstrated. Although not inhibited by TOFA, acetyl-CoA carboxylase is inhibited by TOFyl-CoA. It is proposed that many of the metabolic effects of TOFA in isolated adipocytes can be explained by TOFyl-CoA inhibition of acetyl-CoA carboxylase. TOFA inhibits glycolysis as a secondary event with the primary event of inhibition of fatty acid synthesis causing an accumulation of citrate which is an inhibitor of phosphofructokinase.     

Metabolic transformation of intracraneally injected [1-14C]linoleic and [1-14C]α-linolenic acids in malnourished developing rats

The effect of a low protein diet during pregnancy and lactation on the fatty acid composition of phosphatidylcholine (PC) and phosphatidylethanolamine (PE) from brains of ten-day-old rats was studied. The results indicated that partial deprivation of protein during early development was associated with an increase in the fatty acids of the n−9 family in PC. The fatty acids of the linoleic acid series decreased in PE but were not modified in PC. These minor changes did not affect the double bond index values either in PC or in PE. The effect of protein depletion on thein vivo metabolic transformation of intracraneally injected [1-¹⁴C]linoleic and [1-¹⁴C]α-linolenic acids was also studied. The percentage distribution of the labeled precursors and their derivatives among PC and PE differed from that of mass distribution. These results indicate that the direct uptake of polyunsaturated fatty acids from the blood and/or the low turnover rate of these acids incorporated into PC and PE might be involved in maintaining the fatty acid pattern of these brain lipids.     

Allylic hydroxy fatty compounds with Δ5-, Δ7-, Δ8-, and Δ10-Unsaturation

Several novel allylic mono- and dihydroxy fatty compounds were synthesized from Δ5, Δ7-, Δ8-, and Δ10-monounsaturated fatty acids with the selenium dioxide/tert-butyl-hydroperoxide. Chainlengths were C₁₉ for Δ7 and Δ10, and C₂₀ for Δ5 and Δ8 compounds. With a full range of Δ5- to Δ11-unsaturated allylic monohydroxy fatty compounds available, position-dependent effects in the¹³C-nuclear magnetic resonance spectra of these compounds are discussed. The olefinic carbon shift differences in monohydroxy compounds, where the OH group is located between the double bond and the terminal methyl group, were plotted as a function of double-bond distance from C₁. This plot is presumably a rational function. During SeO₂-based hydroxylation, lactonization of the hydroxy groups, located between the double-bond and the carboxyl group, also occurs for Δ5 unsaturation.     

Absorption and effects of 3-(N-phenylamino)-1,2-propanediol esters in relation to toxic oil syndrome

Toxic Oil Syndrome (TOS) was an epidemic disease related to the consumption of rapeseed oil denatured with aniline that made its sudden appearance in Spain in 1981. The fatty acid esters of 3-(N-phenylamino)-1,2-propanediol (PAP), which is a chemical class of by-products resulting from the reaction of aniline with oil components, have shown a strong association with TOS-related oils. These compounds also show some structural similarities to platelet-activating factor (PAF). In search of a toxic agent that could explain the widespread systemic effects observed in TOS patients, we investigated the intestinal absorption and biotransformation of the different PAP esters found in TOS-related oil samples and the possible pathophysiological effect of these mediators and their metabolic products if acting as PAF analogs. Results indicate that PAP esters are absorbed in the gastrointestinal tract and are distributed and stored in different organs, particularly in the liver and brown adipose tissue. PAP in these organs showed different patterns of fatty acids, indicating the ability of the gastrointestinal tract to modify the fatty acid composition of the parent PAP. Thus, the fatty acid profile of the PAP esters found in intestine appears to be related to the type of oil used as vehicle. Some of these PAP esters, when a long acyl chain was present in the sn-1 position of the molecule, showed an inhibitory effect on the PAF synthesis. This is an important observation in line with the systemic nature of the disease.     

Facile and Stereoselective Synthesis of (Z)-15-Octadecenoic Acid and (Z)-16-Nonadecenoic Acid: Monounsaturated Omega-3 Fatty Acids

Facile syntheses of the monounsaturated omega-3 fatty acids, (Z)-15-octadecenoic acid and (Z)-16-nonadecenoic acid, are presented. Commercially available hydroxy fatty acids were esterified and oxidised, followed by the Wittig reaction to introduce the omega-3 olefinic bond; hydrolysis yielded the omega-3 fatty acids in high purity. An examination of different reaction conditions for the Wittig step found that THF as solvent and coupling temperatures of ?78 °C gave optimal stereoselectivity, affording the omega-3 olefins in Z:E ratios ≥97:3. The syntheses have overall yields of ~43%, and utilise straightforward, robust chemistry, that may be readily scaled up and reproduced. Also presented is a method for accurately determining the double bond geometry and isomeric purity of the fatty acid products using ¹H–¹³C-HSQC NMR and GC–MS, respectively.     

Fettalkoholethoxylate mit eingeengter Homologenverteilung - Entwicklung neuer Alkoxylierungskatalysatoren

Fatty Alcohol Ethoxylates with Narrow Range Homologue-Distribution - Development of New Catalysts for Alkoxylation Fatty alcohol ethoxylates are most important within the group of nonionic surfactants. They are manufactured by acid or basic catalyzed reaction of fatty alcohols with ethylenoxide. The product composition, particularly the homologue distribution, depends on the nature of catalyst. Basic catalysts, which are widely used in technical processes, yield products with a broad range homologue distribution. Three new catalysts for alkoxylation are presented, which yield fatty alcohol ethoxylates with narrow-range homologue distribution. These narrow-range ethoxylates exhibit new interesting properties.     

Fettchemische und petrochemische Rohstoffe - Gegensatz oder Ergänzung?

Fatchemical and Petrochemical Raw Materials - Contrast or Complementation? Fatchemical products are used in all branches of industry and crafts for a variety of purposes. The areas of application are determined by the types of fatty acids which are available as raw materials. It is shown that the C₁₈ chain length is dominant. The most commonly occurring fatty acids are oleic- and linoleic acids. Lauric acids, which is so important for the major areas of application, only represents a small fraction of the world supply of fats. The use of raw material alternatives instead of fats is explained by the relative uniformity of the fatty acid spectrum found amongst the natural fatty acids. In addition, the special place occupied by coconut oil is economically attractive. A survey of the various possibilities and processes for fatchemical products which are derived from fats and petrochemical derivatives is presented. It may be expected that further positive developments of agricultural oil. and fat-production will occur by better yields as well as by successful breeding, resulting in changes in the fat composition. In the long term it may be assumed that the range of natural fats will not only expand, but that it will also be widened by new fatty acid compositions. Petrochemical processes can also have good prospects for the future. Fatchemical and petrochemical raw materials can complement each other in a positive fashion thus enriching the spectrum of fatchemical products.