Synthesis and Bio-activities of Pyrazolyl or Pyridinyl Substituted Tonghaosu Analogs

11 pyrazolyl or pyridinyl substituted tonghaosu analogs were synthesized. Structures of all the new compounds were confirmed by ^1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against larvae of large white butterfly （Pieris brassicae L.）, larvicidal activity toward mosquito （Culex quinquefasciatus Say） and growth control activity toward larvae of Spodoptera litura Fab were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z-1. Based on the activity data, the preliminary structure-activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.     

Synthesis and Biological Activity of Tonghaosu Analogs Containing Phenoxy-phenyl Moiety

A new series of phenoxy-phenyl moieties containing tonghaosu analogs with varied B-ring 9 were synthesized and characterized by spectral studies. Their insect antifeedant activity against Pieris brassicae and insecticidal activity against Culex quinquefasciatus were investigated. Compound 9e exhibited excellent antifeeding activity.     

Synthesis and Antifeeding Activity of Acetylene-Containing Tonghaosu Analogs

During our continuous efforts towards the search for environmental benign insect antifeedant, we established a concise method for the synthesis of Tonghaosu, a naturally occurring antifeedant.[1] Herein, we report the synthesis and antifeeding activity of 22 new tonghaosu analogs, which contain varied B ring as well as one or two acetylene functionalities. Preliminary bioassay indicates that two acetylene groups containing tonghaosu analogs have better antifeedant activity against large white butterfly (Pieris brassicae L.) than those with one acetylene group. More interestingly,Z-isomers are much more active than their corresponding E-isomers.     

Synthesis,Structure and Reactivity of Lanthanocene Complexes

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Synthesis and Biological Activity of Philanthotoxin Analogs

Sodium ion channels, acetylcholine esterase and neurotransmitter receptors in insect neurons and skeletal muscles are often made as target by practical neurotoxic pesticides. But insects can create resistance after using a pesticide for a long time. So th…     

Synthesis and Structure of Tetraphenylglycolide

1 INTRODUCTION Polylactide usually synthesized by a con-densation reaction of glycolide is a kind of use-ful medical polymer. Several structures of gly-colide derivatives have been determined by X-ray diffraction[1], and their molecular struc-tures showed the significant influence of subs-tituents on the conformation of glycolide hete-rocycle. The title glycolide derivative has beenrecently synthesized in laboratory, and its X-ray structure is presented herein to compare themolecular stru…     

Synthesis of the Analogs of Triptolide： 7, 8-Deoxytriptolide, 7 α, 8α-Epoxytriptolide and Related Ketones

Two novel analogues of triptolide were synthesized using triptolide as the starting material through reductive opening of epoxy ring, hydration and olefin epoxidation, and related ketones have also been afforded by oxidation of them with IBX or Jone‘s reagent.     

Study on Synthesis and Intercalation Behavior of Layered Zirconium Proline-N-methylphosphonate-phosphate

Zirconium proline-N-methylphosphonate-phosphate (α-ZPMPP) was prepared in the presence of HF for the first time. The α-ZPMPP sample is highly crystallized with interlayer distance of 1.52nm. The interlayer distance of complex of α-ZPMPP with n-butylamine (α-ZPMPP-BA) is in 0.45 nm larger than that of α-ZPMPP. The α-ZPMPP possesses different intercalation behavior of host-guest compound from α-ZP.     

Study on the Total Synthesis of Ecteinascidin 743 and Its Analogues-Construction of A Pentacyclic Intermediate

A concise and efficient synthesis of the pentacyclic intermediate 1,as a simple model compound of Ecteinascidin 743 and its analogues,is described.     

Study on Synthesis and Electrochemical Properties of Nanophase Li-Mo-spinel

Li-Mn-spinel was synthesized using the rheological phase recation method,First,the precursor was prepared by rheological phase reaction.The it was decomposed to form Li-Mn-spine,which was characterized by X-ray diffraction analysis and IR spectra.The particle size of Li-Mn-spinel was determined by the method of the transmission electron microscopy.The synthesized materials are of nanometer size with 30-100nm in the average diameter.The electrochemical properties of the Li-Mn-spinel were also studied.It proved that this method not only provided a simple practicable and effective route for the synthesis of Li-Mn-spinel,but also had many advantages such as lower sintering temperature,shorter sintering time,fine particles and particularly excellent electrochemical performances.     

新型茼蒿素类似物的合成和抗虫构效关系研究

Twenty-one tonghaosu analogs were synthesized via hydroamination or selective reduction of the endocyclic double bond of the corresponding dienol spiroketals. Structures of all the new compounds were confirmed by ^1H NMR, IR, MS, HREIMS or elemental analysis. Their antifeedant activity against large white butterfly （Pieris brassicae L） and larvicidal activity toward mosquito （Culex quinquefasciatus Say） were examined. Some of them exhibited antifeeding activities comparable to or stronger than tonghaosu Z-1. Based on the activity data, the preliminary structure-activity relationship was also discussed, which might be instructive for finding out lead compounds with better bioactivities in the future.     

Analysis of Volatile Organic Compounds from Dendranthema indicum var. aromaticum by Headspace Gas Chromatography-Mass Spectrometry and Accurate Mass Measurement

The volatile organic compounds from flowers, leaves, and stems of Dendranthema indicum var. aromaticum, obtained through a static headspace technique, were analyzed by gas chromatography-mass spectrometry (GC-MS) and accurate mass measurement. The qualitative approach, comprising accurate mass measurement, retention index, and mass spectral search, was utilized to identify compounds. A total of 162 components were identified, representing 97.55–98.72% of the volatiles of individual samples. The principal chemical components in flowers were bornyl acetate (15.40%), α-phellandrene (14.18%), p-cymene (9.64%), camphor (9.54%), β-linalool (8.61%), and α-thujone (7.06%). In leaves, the main components were p-cymene (20.42%), bornyl acetate (20.41%), α-phellandrene (13.67%), and β-linalool (5.46%). As for stems, trans-β-farnesene (17.95%), germacrene D (12.89%), β-phellandrene (12.70%), β-caryophyllene (10.18%), and bicyclogermacrene (8.01%) were the dominant volatile compounds. Comparative studies on the volatiles from various species of genus Dendranthema indicated that Dendranthema indicum var. aromaticum contains significantly more aroma compounds than its morphologically similar species.     

前列环素(PGI2)及其类似物的合成

本文综述了前列环素及其类似物的合成。类似物包括有7-羰基—、10,10-二氟—、5-氯—,4-羰基—、6,9-硫—、6,9-氮—,6 a-碳—前列环素以及苯前列环素等。前列环素及其类似物是一类具有抑制血小板聚集的生物活性化合物。     

Efficient Synthesis of Thalifoline and Its Analogs

Thalifoline (1) and its analogs were synthesized from methyl 3-hydroxy-4-methoxy benzoate by prenyl etherification, Claisen rearrangement, oxidation, imine formation, reductive amination and intramolecular amidation. The last three steps, imine formation, reductive amination, and intramolecular amidation, were completed in one pot at room temperature.     

Taxol: Synthesis,Bioactive Conformations,and Structure-Activity Relationships in Its Analogs

The review describes the syntheses and probable biologically active conformations of taxol, a natural antitumor agent, and systematizes published data on the structure-activity relations in the series of taxol analogs.__________Translated from Zhurnal Organicheskoi Khimii, Vol. 41, No. 3, 2005, pp. 329–362.Original Russian Text Copyright © 2005 by Zefirova, Nurieva, Ryzhov, Zyk, Zefirov.Dedicated to Full Member of the Russian Academy of Sciences V. I. Minkin on his 70th Anniversary     

利用高效液相色谱鉴定化学合成的 δ-睡眠诱导肽及其类似物

用高效液相色谱对化学方法合成的δ-睡眠诱导肽(DSIP)及其类似物(Tyr~1-DSIP,Phe~5-DSIP以及Tyr~1Phe~5-DSIP)的主要成份进行了分离,应用在线的紫外光谱和萤光光谱检测,并将分离出的色谱峰收集后进行氨基酸分析。     

Facile Synthesis of Isodamascone and Its Analogs

Synthesis of isodamascone and its analogs, the commercially important aroma compounds, have been accomplished from the readily available 1,5,5‐trimethyl‐2‐cyclohexen‐1‐ol via a short, facile, and simple sequence of reactions in excellent yield.     

Sulforaphane and Its Bifunctional Analogs: Synthesis and Biological Activity

For decades, various plants have been studied as sources of biologically active compounds. Compounds with anticancer and antimicrobial properties are the most frequently desired. Cruciferous plants, including Brussels sprouts, broccoli, and wasabi, have a special role in the research studies. Studies have shown that consumption of these plants reduce the risk of lung, breast, and prostate cancers. The high chemopreventive and anticancer potential of cruciferous plants results from the presence of a large amount of glucosinolates, which, under the influence of myrosinase, undergo an enzymatic transformation to biologically active isothiocyanates (ITCs). Natural isothiocyanates, such as benzyl isothiocyanate, phenethyl isothiocyanate, or the best-tested sulforaphane, possess anticancer activity at all stages of the carcinogenesis process, show antibacterial activity, and are used in organic synthesis. Methods of synthesis of sulforaphane, as well as its natural or synthetic bifunctional analogues with sulfinyl, sulfanyl, sulfonyl, phosphonate, phosphinate, phosphine oxide, carbonyl, ester, carboxamide, ether, or additional isothiocyanate functional groups, and with the unbranched alkyl chain containing 2–6 carbon atoms, are discussed in this review. The biological activity of these compounds are also reported. In the first section, glucosinolates, isothiocyanates, and mercapturic acids (their metabolites) are briefly characterized. Additionally, the most studied anticancer and antibacterial mechanisms of ITC actions are discussed.