Synthesis and Fungicidal Activities of 2-Alkylthio-5- （3, 4, 5-tribenzyloxyphenyl）-1, 3, 4-oxadiazoles

Abstract： Ten novel 2-alkylthio-5-（3, 4, 5-tribenzyloxyphenyl）-1, 3, 4-oxadiazole derivatives （5a-j） were synthesized from methyl 3, 4, 5-trihydroxybenzoate by ethedfication, hydrazidation, cyclization and thioetherification reactions. The structures of 5a-j were confirmed by 1HNMR, MS spectra and elemental analysis. The results indicated that most of the compounds 5 exhibited good fungicidal activities. The activity of 5h is higher than 90% against Fusarium oxysporum and Botrytis cinereapers in 50 mg/L.     

Chemoenzymatic synthesis of (4S,5R)-5-hydroxy-γ-decalactone

Reduction of ethyl 2-hydroxy-3-oxooctanoate with immobilised baker's yeast at pH 4.0 yields anti-2R,3R-dihydroxy ester with high diastereoselectivity and enantioselectivity (de 70%, ee 80%) which is conveniently converted to (4S,5R)-5-hydroxy-γ-decalactone.     

Asymmetric Synthesis of （-）-（4R, 5R）-4-[5-（Benzo[1, 3]dioxol-5-yl）-4- hydroxyl- 1-（pyridin-2-yl）-4, 5-dihydro- 1H-pyrazol-3-yl]benzamide

For discovering novel small molecule inhibitors of transforming growth factor-β1(TGF-β1)type-I receptor(ALK5),we designed1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole(1)as target compound,mimic the structure of SB-431542which is a2-pyridyl substituted triarylimiazole inhibitor of ALK51.Racemic compound1showed moderate ALK5inhibitory activity in luciferase reporter assays[inhibition(%control):0.1umol/L8.79%;1umol/L19.05%].To investigate the influence of the absolute configuration of…     

Synthesis of (4R,5S)-(−)- and (4S,5S)-(+)-L-Factors and Muricatacin from D-Glucose

Abstract

In connection with our projects on the synthesis of biologically active 5-hydroxyalkan-4-olides which have a chiral 2.3-diol unit,¹ we have carried out the synthesis of (4R,5S)-(?)- and (4R,5S)-(+)-L-factors (1).² the proposed autoregulators from Streptomyees griseus, and muricatacin (2),³ a biologically active constituent from the seeds of Annona muricata L. via 2.3-dihydroxy aldehydes derived from D-glucose. Hex-3-enofuranose4 was prepared by the elimination of thetriflate derived from D-glucose.     

5-丁基-9-苯基-4, 5, 6, 9-四氢苯并[d, e]恶唑[5, 4-g]-异喹啉-4, 6-二酮的合成

本文给出了一条较好的制备5-丁基-9-苯基-4, 5, 6, 9-四氢苯并[d, e]恶唑[5, 4-g]-异喹啉-4, 6-二酮的反应路线, 即: 先由4-溴-1, 8-萘酐经亚胺化、硝化、水解和还原等反应制得N-丁基-3-硝基-4-羟基-1, 8萘酰亚胺, 再在硼酸的存在下, 将亚胺与苯甲酰氯反应可得到目标化合物。文中给出了该化合物的质谱、核磁共振、红外、紫外和荧光等光谱数据。     

(4R,5S)-5-羟基-4-甲基-3-己酮的合成

农业害虫药材甲Stegobium panicem Linnae在我国各省区都有分布,主要危害谷类、食品、药材、图书、档案等.我国一般每年可以发2～3代,温度较高的地区可发生4代[1] .     

Synthesis and Molecular Structure of 5, 5-Dimethyl-2- (4' -methoxy)phenyl-1, 3, 2- thiazaphospholidine-4-thione 2-sulfide

1 INTRODUCTION In our previous study [1], we found that 1, 3, 2-thiazaphospholidine-4-thione 2-sulfide deriva- tives possessed various bioactivities such as herbicidal, antiviral, fungicidal activity, Which the is strongly held our interest to exploit new method for the synthesis of such phosphorohe- terocycles and investigate their biological activities. Different method for the preparation of 1, 3, 2-thiazaphospholidine-4-thione (one) 2-sulfides have been reported [2~4]. According to …     

Regioselective and Stereoselective Synthesis of the 3-Aryl-4- phosphoryl-1, 2, 4-triazoline-5-ones

Regioselective cyclization of 1-acylthiosemicarbazides has been shown to be an excellent method for the synthesis of triazoles, thiadiazoles and oxadiazoles, with a variety of potential biological activities1-6 and utilities as pharmacological properties7…     

Asymmetric Synthesis of （S）-Dimethyl -4, 4＇-dimethoxy-5, 6, 5＇, 6＇-dimethenedioxybiphenyl-2, 2＇-dicarboxylate

(S)-Dimethyl-4, 4‘-dimethoxy-5, 6, 5‘, 6‘-dimethenedioxy-biphenyl-2, 2‘-dicarbonylate was synthesized in reasonable yield through a series of reactions, including chiral oxazolinemediated asymmetric Ullmann coupling, from methyl 2-bromo-5-methoxy-3, 4-methenedioxybenzoate.     

Total Synthesis of Two 4, 5-Dioxo-seco-eudesmane Sesquiterpenes

A facile synthetic route to two seco-eudesmane, 4, 5-dioxo-10-epi-4, 5-seco-γ-eudesmane (1) and 4, 5-dioxo-10-epi-4, 5-seco-γ-eudesmol (2) from ( )-dihydrocarvone has been described. Avoiding expensive reagents, this highly economic method especially suits for the synthesis of 4, 5-seco-eudesman-type and ophianon-type sesquiterpenes with a double bond at position 11 and 12.     

A convenient chiron approach to (4R,5R)-5-hydroxyalkylbutan-4-olides and the corresponding 7-oxa analogues from d-(+)-mannitol via an advanced common precursor: syntheses of (−)-muricatacin, 7-oxa-(−)-muricatacin, (4R,5R)-(−)-5-hydroxy-4-decanolide,and (4R,5R)-(−)-7-oxa-5-hydroxy-4-dodecanolide

An efficient and concise chiron approach toward the synthesis of (−)-muricatacin and its unnatural 7-oxa analogue starting from commercially available and inexpensive d-(+)-mannitol via an advanced common chiral precursor has been described. In addition, (4R,5R)-(−)-5-hydroxy-4-decanolide and (4R,5R)-(−)-7-oxa-5-hydroxy-4-dodecanolide were also synthesized to show the versatility of this synthetic strategy. The methodology involves the conversion of a common chiral intermediate, prepared from d-(+)-mannitol in six steps, to a variety of target molecules in only two steps.     

面包酵母对1, 4, 4α, 8α-四氢-1, 4-亚甲基萘-5, 8-二酮的催化异构化

文章描述了面包酵母将1, 4, 4α, 8α-四氢-1, 4-亚甲基萘-5, 8-二酮催化异构化为1, 4-二氢-5, 8-二羟基-1, 4-亚甲基萘, 而不是还原为相应的羟基化合物。     

Synthesis of 1, 4-Bis[3-N-propionyl-2-aryl-1, 3, 4- oxadiazoline-5-yl]phenylenes

1, 3, 4-Oxadiazoline derivatives are found to possess significant biological activities such as antifungal1, insecticidal2, CNS depressant3-5, anticonvulsant effects and plant growth accelerator. They are highly important heterocycles, and have been used …     

3, 5-二氢-4H-咪唑啉-4-酮的合成

通过膦亚胺(2)与芳基异氰酸酯的aza-Wittig反应得碳二亚胺(3),再应用3与亲核试剂的成环反应制得了8个2-氨基取代咪唑啉酮的新衍生物5a～5h。探讨了碳二亚胺3与不同亲核试剂反应的活性。     

Synthesis of 2s, 4s, 5s -dihydroxypipecolic acid and bulgecinine [2s,4s,5r-4-hydroxy-5- (hydroxymethyl)proline] from d-glucuronolactone,a strategy for the synthesis of 2s,4s-4-hydroxy-α-amino acids

The efficient synthesis of 4S,5S-2-(N-benzyloxycarbonyl)amino-5,6-dihydroxyhex-2-en-4-olide (4) from D-glucuronolactone is described, the potential of (4) as a divergent intermediate for the synthesis of 2S,4S-4-hydroxy-α-amino acids is illustrated by the conversion of (4) to 2S,4S,5S-dihydroxypipecolic acid and bulgecinine [2S,4S,5R-4-Hydroxy-5-(hydroxymethyl)-proline].     

Synthesis and Crystal Structure of 2-Amino-3-ethoxycarbonyl-4-（4-chlorophenyl）-4H, 5H-pyrano-[3,2-c]-benzopyran-5-one

1 INTRODUCTION The coumarins constitute an important class of bioactive natural products[1]. They have been found to possess diverse biological properties including antimicrobial, insecticidal, estrogenic, anticoagulant and antithrombotic activities. Som…     

Studies on Selena-Macrocyclic Amides Synthesis and Structural Characterization of 7-Phenyl-5, 9-dioxo-1-selena-4, 7, 10-triazacyclododecane and 6-(4-Nitrobenzyl )-5, 9-dioxo-1, 4, 7, 10-selenatriazacyclododecane

lmTR0DUCTI0NSincetheseleniumcoronandswereachivevedin1989tli,thesynthesisandcoor-dinationchemistrystudyofthismacrocycliccomPOundshavereceivedwideattentionowingtotheirstrongcomplexingabilitiestowardssoft.transiti0nandheavymetals.InourprevibuspaPer,wereP0rtedthecrystalstructureoftw0selenacrownethers(2'3)andaPd(1)complexwith10'selenabenzo-15-crown-5t4i.Duetothedifficultyofthepreparationsofselenium-nitr0genmixeddonorc0n-..tainingmacrocycles,thestudyontheseligandsisconsiderablyscarce.Thesynthes…     

Crystal Structure of 3, 4-trans-4, 5-trans-2-Amino-3-cyano-1, 3-diethyloxy carbonyl- 4, 5-di (4-chlorophenyl)cyclopentene

1INTRoDUCT1oNThechemistriesofsamariumdiiodideandlow-valenttitaniumareofcurrentin--.terestinorganicSynthesis.Theyhavebeenwidelyusedinsyntheticreactions(l.2i.Thereactivityofthereagentstowardsvariousnitrogen-containingcomPOundshasal-readybeenexamined.Thereare,toourknowledge,noliteratureexamplesforthereductionofafylidenecyanoacetatederivativeswiththesereagents.Recently,wefoundthatthetitlecompoundisobtainedbycyclodimerizationreactionofpchlorObenzylidenecyanoacetatewithsamariumdiiodideorlow-va…     

(2S, 3R, 4R)-4, 5-O-异亚丙基-2, 3-环亚硫酰-2, 3, 4, 5-四 羟基戊酸乙酯 中硫原子手性的研究

我们在合成鞘氨醇3时,成功地分离到一对环亚硫酸酯1由于硫原子手性形成的非对映异构体,通过氢核磁共振谱分析和分子力学计算,确定了它们手性硫原子的绝对构型.     

(2S, 3R, 4R)-4, 5-O-异亚丙基-2, 3-环亚硫酰-2, 3, 4, 5-四 羟基戊酸乙酯 中硫原子手性的研究

我们在合成鞘氨醇3时,成功地分离到一对环亚硫酸酯1由于硫原子手性形成的非对映异构体,通过氢核磁共振谱分析和分子力学计算,确定了它们手性硫原子的绝对构型。