Total Synthesis of (±)-Nimbonone and (±)-12-Ethyl-13-methoxy- 8,11,13-podocarpatriene

Most diterpenoids exhibit significant bioactivities, such as antidermatophytic, antibact- erial, and antioxidant. Although a large number of aromatic tricyclic diterpenoids have been isolated, there are a few of them having ethyl substituent. The synthesis of this type diterpenoids has been seldom reported. In order to further study the relationship between the structure and bioactivities of the diterpenoid, we extended the diterpene synthesis1,2,3. It is desirable to report herein the syn…     

First Total Synthesis of (±)-13-Hydroxy-8 (14)-abietene

(±)-13-Hydroxy-8 (14)-abietene, a rare alicyclic diterpene possessing an isopropyl group and a hydroxy group at the C-13 position, was isolated from Solidago missouriensis nutt1. Many diterpenes exhibit significant bioactivities, such as antibacterial. As a part of our synthetic studies on the naturally-occurring diterpenes, we are attemping the synthesis of the rare natural compound. To our knowledge no total synthetic work has been reported yet. In order to study the further relationship b…     

Concise Synthesis of(±)-epi-Chrysotricine

Chrysotricine 1 was isolated from the Chinese herb medicine Hedyotis Chrysotricha and was shown to possess antitumor activity1. Its structure has been elucidated as a novel zwitterionic (-carboline alkaloid containing a 2,2,5-trisubstituted tetrahydrofuranyl group. The (-carboline compounds have attracted considerable attraction in recent years because of their promising and intriguing biological activities2. Recently, we have established the absolute configuration of chrysotricine by the fir…     

Facile and Efficient Syntheses of (±)-2,6-Dimethyl-6-hydroxy-2,7-octadienoic Acid and Its Methyl Ester

IntroductionMonoterpenoid acid 7a,which is a componentof some traditional medicines such as Gymnocladuschinensis baillon in a glycoside form[1— 3 ] ,has re-cently been isolated from Artemisia sieberi in Iran ina free form[4] .The structure ofthe compound7a has been es-tablished to be( E) - 2 ,6- dimethyl- 6- hydroxy- 2 ,7-octadienoic acid by chemical and spectroscopic anal-yses.Its methyl ester derivative7b was isolatedfrom the antibacterial extracts of the leaves ofPiper aduncum as well[5]…     

A Novel Total Synthesis of (±)Shikonin

Shikonin 1 was a key component isolated from the traditional Chinese herbal medicine, Zicao(Lithospermum erythrorhizon Sieb.et Zucc), which possesses multiple biological activities1. There have been many synthetic routes to shikonin, however, all these ro…     

(±)-Yaequinolone A2的简洁全合成

由廉价的邻氨基苯甲酸为起始原料经6步反应以27.8%的总产率首次合成了2-喹啉酮类生物碱(±)-yaequinolone A2,关键步骤为MOM保护的α-羟基酰胺进行的高非对映选择性分子内aldol 反应。     

Studies on Macrocyclic Diterpenoids (Ⅵ)——A Novel Synthetic Route to (±)-Cembrene-A

The total synthesis of(土)-cembrene-A, a termite pheromone, was achieved from geranylacetone and geraniol as starting materials. The key steps were the phase transfer catalyzed coupling reaction of sulphone (6) with chloride (9) and the intramolecular macrocyclization of dicarbonyl precursor (12) induced by low valent titanium. The synthetic route was short with anoverall yield of 17%.     

两种新木脂素(±)-Eusiderin E和(±)-Eusiderin F的全合成研究

以焦性没食子酸为原料 ,以克来森重排为关键步骤 ,首次合成了天然产物 (± ) -Eusiderin E和 (± ) -Eusiderin F     

Synthesis of Gingerenone C and 5-Hydroxy-1-(4′-hydroxy-3-methoxyphenyl)-7-(4′′-hydroxyphenyl)-3-heptanone

Diarylheptanoidsconstituteadistinctgroupofmetabolitesofnaturalplantcharacterizedbytwoaromaticringslinkedbyalinearsevenaliphaticchain.Therehavebeenfewreportsonthebiologicalactivitiesofdiarylheptanoids,mostofwhichappearingintheareasofanti-inflammatory,anti-oxidative,superoxidescavengingandanti-hepatotoxiceffects1,2.SomeofthemareusedastraditionalmedicineinAsia3.Compound1and2werefirstlyisolatedfromtherhizomesofZingiberofficalrespectively4,5.Sofarthesynthesisofthesetwocompoundshavenotbeenreportedy…     

A Convenient Synthesis of cis and trans-(±)-4-Amino-1-[2-(hydroxyl-methyl)-1,3-oxathiolan-5-yl]-2(1H)-pyrimidinone

A convenient synthesis of cis-(±) isomer 1 and trans-(±) isomer 2 of lamivudine starting from benzoyloxyacetaldehyde and l,4-dithiane-2,5-diol is described. The key steps include chlorination of oxathiolane lactol 5 by SOCl2/DMF, followed by coupling with silylated N4-acetylcytosine and deprotection. The overall yield was 42.6 % and 20.1 %, respectively.     

Efficient and Facile Synthesis of ( ± )-Salvirecognine

Salvirecognine (7) is a diterpene isolated from Salvia recognita[1] which has been the subject of continued and growing interest, due to the range of biological activities shown by many members of this family. [2] In order to study further relationships between the structure and biological activity of the diterpene compounds and as an extension of diterpenoid synthesis in our laboratory, [3,4] the first total synthesis of the title compound was achieved by an efficient and facile route (Scheme 1).     

Synthesis and Properties of Three Tris(1,10-phenanthroline) ruthenium (Ⅱ) Derivatives

MThekeymaterials,5-amino-l,10-phenanthrolineandetS-Ru(phew,CI,,werepreparedbythemethodsofreferences"'.Synthesisofla,foandicEquimolaramountsofcorrespondingto-bromo-alkyIacyIohIondewasaddeddropwisetoasuspensionof5-amino-l,10-phenanthrolineandsodiumdicarbonateindryacetonitrilewithstirringatroomtemperatureundernitrogenfor4-6hours.Thentheresultingsolidwasfilteredandwashedbyacetonitrile,5%sodiumbicarbonateaqueoussolutionandwaterinturn.Afterbeingdriedicvacuo,yellowmicrocrystalsla-cwereobtained.Sy…     

Total Synthesis of (±)-Celaphanol A

Celaphanol A was a diterpene isolated from the stems of Celastrus stephanotifolius1, which have been the subject of continued and growing interest, due to the range of biological activities shown by many members of this family2. Some have been used in traditional medicine3 or as a stimulant4 from ancient times. In order to further study the relationship between the structure and biological activity of the diterpene compound and as an extension of diterpenoid synthesis in our laboratory5, 6, …     

Synthesis and Properties of D-Thymidylyl (3'→5')L-Thymidine (D/L-TpT)

Inrecentyearsmuchefforthasbeenspenttodevelopoligonucleotideanalogsashighlyselectivepharmaceuticalagentstoblockexpressionofdisease-associatedproteins'-'.andtheseefT'ortshaveresultedilltheapprovaloffomiversensodium(vitravene',"),thefirstantisensedrug,byFDAinAugust1998fortreatmentofAIDSpatientswithcytomegalovirus(CMV)-inducedretinitis6.However,thegreatpotentialofantisenseoligonucleotidesasantiviralandanticanceragentsiscompromisedbytheirnucleasesusceptibilityandlowcellmembranepermeability.L-D…     

Adsorption and Reaction of CO on Mo(100)-c(2×2)-N Surface Studied by HREELS

Molybdenum nitrides have attracted significant attention recently due to their uniquephysical and chemical properties. Many studies have shown that Mo,N is an activecatalyst for CO hydrogenation. The fundamental understanding concerning the reactionmechanisms over Mo=N. however, is not well established. The powerful surface sciencetechniques may provide an insight into the surface structure and properties of such animportant catalytic material. In previous paper', we described the results o…     

First Total Synthesis of 5_α-Hydroxy-isopterocarpolone

Sesquiterpenic compounds of the Eudesmane family have attracted considerable attention due to their intriguing biological properties1,2, particularly significant antifeedant activity, cell growth inhibitory and plant growth regulating activities.In 1996, J. Hu and co-workers3 had isolated eudesmane sesquiterpene 5?-hydroxy-isopterocarpolone 1 from the aerial parts of chinese folk medicine Artemisia eriopoda and elucidated its structure by spectropic methods. Herein, we reported the first tota…     

Total Synthesis of (±)Chrysotricine

Chrysotricine1wasisolatedfromtheChineseherbmedicineHedyotiSChrysotricha'anditssthectUrehasbeenestablishedasanew0-carbolinealkaloidwitha2,5-trans-substitutedtetrahydrofuranylgrouPatitsl-positionbyX-raydiffractionandspectralanalysis.PharmaceuticalstUdiesshowedpotentialantitUmoractivity.Theinterestingbiologicalactivityandthechemistryof6-carb0linesmict[JIehaveattiactedconsiderableattentioninrecentyears.InordertostUdythisstrUctUre-activityrelationshiPfurther,wewereillterestedinthedevelopmento…