取代苯基呋喃甲酸长链烷基酯的合成及生物活性

取代苯基呋喃甲酸长链烷基酯的合成及生物活性司宗兴＊孙亚秋汪海涛（中国农业大学应用化学系北京１０００９４）关键词苯基呋喃甲酸酯，合成，杀菌活性１９９６－０６－１７收稿，１９９６－１２－０５修回取代芳基呋喃甲酸是一类很好的活性基团，它的酯在医学上用做镇痛...     

Exotic Amino Acids. 8. Synthesis of Monomethyl Esters of N-Arylaminomethylenemalonic Acids

N-Arylaminomethyleneisopropylidenemalonates, obtained from ethoxymethyleneisopropylidenemalonate and aromatic amines, underwent methanolysis to form monomethyl esters of N-arylaminomethylenemalonic acids. The conditions of their formation and their yields depend on the nature and positions of the substituents in the aromatic ring of the initial amine.     

全氟烷基芳基酮的合成

本文用8种取代苯基卤化物,在无水四氢呋喃中制成的格氏试剂与全氟羧酸(R_FCO_2H,R_F=CF_3和n-C_3F_7)按 3:1摩尔比反应,合成了9种全氟烷基芳基酮(1～9),其中6、7、8和9是新化合物。它们的结构用IR、UV、NMR(~1H,~(19)F)及MS加以表征。     

新型2-苯并噻唑磺酰脲氨基酸及其甲酯衍生物的合成与抗肿瘤活性

以2-巯基苯并噻唑为原料,经弱氧化和氨化制得2-苯并噻唑次磺酰胺（2）; 2经高锰酸钾氧化制得2-苯并噻唑磺酰胺（3）; 3与氯甲酸乙酯反应制得2-苯并噻唑磺酰胺甲酸乙酯（4）; 4与L-氨基酸甲酯反应制得一系列2-苯并噻唑磺酰脲氨基酸甲酯（6a~6j）; 6经水解合成了10个新型的2-苯并噻唑磺酰脲氨基酸（7a~7j）,其结构经¹H NMR, IR和ESI-MS表征。并研究了6和7对Cdc25B的抑制活性。结果表明:在用药浓度为20 μg·mL^-1时,6c, 6j, 7d, 7h和7j对Cdc25B抑制活性较好,抑制率分别为78.1%, 71.2%, 65.6%, 57.2%和65.9%。     

Synthesis and Liquid Crystal Properties of Aryl Esters of Laterally Substituted 5-Pyrimidinecarboxylic Acids

(p-R-phenyl)-4-methyl-, 4-methoxy-, and 4-hydroxy-5-pyrimidinecarboxylates have been synthesized and their liquid crystal properties examined. Compounds containing methyl and methoxy groups in the lateral position of the molecule are nematic liquid crystals with a mesophase range of 30-50°C, but the 4-hydroxy derivatives are smectic liquid crystals. With variants of the substituents in a series of (p-R-phenyl)-4-substituted 5-pyrimidinecarboxylates the mp of individual representatives were successfully reduced by 50°C in comparison with the 4-unsubstituted analogs and the range of the mesomorphic state was extended to 190°C.     

A Simple Method for the Preparation of Substituted Phenoxyacrylic Acid Phenyl Esters

A simple and efficient synthesis of phenoxyacrylic acid phenyl esters via one pot esterification and Michael-type addition starting from propynoic acid and an excess of an appropriate phenol is described.     

取代苯基吡唑类化合物的合成及其除草活性

以1′-(4-氯-2-氟-5-甲基苯基)-4′,4′,4′-三氟-1,3-丁二酮为原料,合成了一系列具有取代苯基吡唑结构的新化合物.化合物结构经¹HNMR,IR,CIMS和元素分析确认.初步生物活性测试表明,所合成的化合物对阔叶杂草具有较高的活性.     

Oxathiaphospholane Approach to the Synthesis of Conjugates of Amino Acids Methyl Esters with Nucleosides

Based upon 1,3,2-oxathiaphospholane chemistry, 5'-O-derivatization of nucleosides with the O-methyl esters of amino acids was performed and corresponding conjugates were obtained in satisfactory yield.     

New Synthesis of Substituted Cyclopropanephosphonic Acid Esters

Abstract

Aminocyclopropane phosphonic acids are considered to be “transition state analogues” of aminocyclopropanecarboxylic acids and they may serve as enzyme inhibitors¹. We attempted to synthesise aminocyclopropane derivatives by a new route². Phosphonoacetic acid allylic esters were subjected to an intramolecular, radical cyclisation in the presence of iodine, solid potassium carbonate and phase transfer catalyst.     

氨基膦酸及其酯的合成

综述了α－氨基膦酸及其酯的合成方法,介绍了近年来发展的不对称合成法,并对各种方法的优劣作了评述。     

Synthesis and Cytotoxic Activity of 1,3,5-Triazinane Derivatives Based on Primary Amines and Amino Acids Esters

Russian Journal of General Chemistry - A series of 1,3,5-triazinane derivatives was synthesized and their cytotoxic activity was studied in vitro on normal cell line (HEK293) and tumor cell lines...     

长链脂肪族二元酸的合成及其在缩聚反应中的应用

长链脂肪族二元酸一般是指含有10个或以上碳原子的饱和直链二元酸,其两端带有羧基官能团,可用于合成香料、特种尼龙工程塑料、热熔胶、涂料、增塑剂、高级润滑油等众多化工产品;由于其链段中含有长烷烃链段,具有优于短链二元酸的性质,使得相应的合成材料具有优越的性能,因此广泛应用于化工、轻工、国防、汽车工业、工程材料等领域;同时,还可用于开发新的聚合物产品。长链脂肪族二元酸在自然界中不单独存在,目前工业上主要通过化学合成法和生物发酵法生产。本文主要对长链脂肪族二元酸的合成方法进行综述,包括传统有机合成、生物技术转化、烯烃复分解、异构化-氢氧羰基化及聚乙烯端基功能化等,并简要概述长链脂肪族二元酸在缩聚反应(聚酯和聚酰胺)中的应用。最后,对合成方法待解决的问题进行了总结,并对未来发展方向进行了展望。     

Synthesis of Phenyl or 4-Nitrophenyl Methyl β-Ketophosphonate Esters

Seven new aryl methyl g -ketophosphonate esters were synthesized. The hydrolytic rates of the compounds under physiological conditions were studied. Most of the compounds are effective inhibitors of acetylcholinesterase. The enzyme recovers on the 10-50 h time scale from its adducts with two of the inhibitors.     

双光气法合成取代苯异氰酸酯

以双光气和取代苯胺为原料，合成了14个取代苯异氰酸酯，产率37．4％－92．3％，并研究了影响反应的各种因素。     

Design,Synthesis and Insecticidal Activities of Novel Phenyl Substituted Isoxazolecarboxamides

Thirteen novel phenyl substituted isoxazolecarboxamides were synthesized, and their structures were characterized by ¹H NMR, elementary analysis and high-resolution mass spectrometry(HRMS) techniques. Their evaluated insecticidal activities against oriental armyworm(Mythimna separata) indicate that the phenyl substituted isoxazolecarboxamides exhibited moderate insecticidal activities, among which compounds 9c and 9k showed comparatively higher activities.     

氟代二苯乙烯氨基酸的合成及性能

以4-碘-L-苯丙氨酸为初始原料,经羧基和氨基的保护得到化合物2;化合物2与4-氟苯乙烯进行Heck反应得化合物3;化合物3脱去保护基得氟代二苯乙烯氨基酸(4,47.4%);其结构经1H NMR,13C NMR,IR和MS(ESI-TOF)确证。光学性质研究结果表明:4的激发、发射波长分别为314 nm和355 nm,斯托克斯位移为41 nm,荧光量子产率为0.22。化合物4在甲醇溶液中存在光致顺反异构现象,反式→顺式结构转变速率常数为0.026 min^-1。     

取代氨乙基膦酸的简便合成

以2-氯乙基膦酸和胺为原料，经一步反应合成了3种取代氨乙基膦酸，合成工艺条件为：2-氯乙基膦酸200mmol，n(2-氯乙基膦酸)：n(胺)=1：1．1，反应温度18℃，反应时间120h，pH8～10，KI作催化剂，收率78．2％～91．0％。用元素分析，IR和^1H NMR表征了标题化合物。