Synthesis of β-L-2′,3′-Dideoxy-2′-fluoro-3′-hydroxymethylarabinofuranosyl Pyrimidine Nucleosides

β-2′,3′-Dideoxy-2′-fluoro-3′-hydroxymethylarabinofuranosylthymine 10 and cytosine 12 were synthesized from L-xylose and were found to be inactive against HIV-1 in acutely infected lymphocytes.     

Synthesis, Crystal Structure and Spectrometry Study of Chiral N-Ethyl-N''''-(2'''',3'''',4'''',6''''-tetra-O-acetyl-β-D-glycosyl)-thiocarbamide

1INTRODUCTIONManynomadicsugarsperformimportantbio-logicalfunctions[1].Theycancontrolvariousgeneexpressionstoadjusttheupgrowth,developmentandreactionoforgans[2].Glycosylisothiocyanateshavebeenwidelyusedasvaluableintermediatesinthesynthesisofglycosylderivatives[3].Theiso-thiocyanatesandglycosylisothiocyanateshavebeenthefocusofsyntheticattentionduringrecentyearsbecauseoftheirpotentialpharmacologicalproperties[4].Theyhavealsoattractedconsiderableinterestduetotheanti-HIVactivityshownby1-deoxy…     

Understanding the Behavior of Thermomyces lanuginosus Lipase in Acylation of Pyrimidine Nucleosides Possessing 2′-Substituent

The effect of 2′-differing substituent groups (such as the H, F, Cl, Br, OCH₃) as well as various chain lengths of the acyl substrates (C6, C10, and C14) on the performance of Thermomyces lanuginosus lipase for the regioselective acylation of pyrimidine nucleoside analogs was investigated systematically for the first time. The results evidently demonstrated that changing substituents in nucleosides had a significant influence on the substrate specificity for the enzymatic reaction, possibly due to the differences in physicochemical properties of the substituents and the special shape of the substrate binding site in enzyme active region. With respect to the chain-length selectivity, the enzyme exhibited the highest 5′-regioselectivity toward the longer chain (C14) as compared to short (C6 and C10) ones. The reason might be attributed to the presence of the interaction between the acyl chain and the large hydrophobic substrate-binding pocket.     

Synthesis and Pharmacological Activity of Annelated Pyrimidine Derivatives

A series of 1-glycosyl-2-glycosylthiopyrimidine (4), annelated pyrimidine derivatives, pyrazolo[3,4-d]-pyrimidine (8), ditetrazolo[1,5-a;1‘,5‘-c]pyrimidine (9), 2,9a,10-triazaanthracene (12), thieno[2,3-d]pyrimidine (14),9-thia-1,3,5,7-tetraazafluorene-8-one (15), 7-oxa-9-thia-1,3,5-triazafluorene-8-one (16), 5-oxa-9-thia-1,3-diaza-fluorene (21a and 21b) derivatives have been synthesized via a sequence of heterocyclization reactions of suitably functionalized 6-[5-(4-bromophenyl)oxazol-4-yl]-1，2，3，4-tetrahydro-2-thioxo-4-oxopyrimidine-5-carbonitrile (2) with different electrophiles and nucleophiles. The new compounds were prepared with the objective to study their pharmacological properties.     

Synthesis of Substituted 3H-Indole-modified β-Cyclodextrin

Substituted 3H-indole modified β-cyclodextrin (β-CD) was prepared by the reaction of 6-deoxy-6-[(2-aminoethyl)amino]-β-CD (CDen) with 2-[(p-amino)phenyl]-3, 3-dimethyl-5-car-boxyl-3H-indole (substituted 3H-indole) in the presence of dicyclohexylcarbodiimide (DCC) and 1-hydroxybenzotriazole (HOBt). The product has been characterized by means of elementalanalysis, MS and ^1H NMR.     

Synthesis of a new 2,2'''':6'''',2''''''''-terpyridine derivative and its coordination property

A novel compound, (E)-4'-(4-(but-1-en-3-ynyl)phenyl)-2,2':6',2'-terpyridine 1 was synthesized from 4'-(4-bromomethylphe- nyl)-2,2':6',2'-terpyridine phosphonium salt 2 and propargylaldehyde via Wittig reaction, and characterized by EI-MS and 1H NMR as well as elemental analysis. The spectral changes of the compound in the presence of transition metal ions, such as Cu(Ⅰ) or Zn(Ⅱ), are investigated.     

Synthesis of New 5‐Substituted Pyrimidine Acyclonucleosides

Acyclonucleosides of pyrimidine were prepared by condensing appropriately silylated 5‐substituted pyrimidines with an acyclic side chain in the form of an acetylated haloalkoxyalcohol and subsequent removal of the protecting acetyl group in base. Also, acyclonucleosides with a 1‐ethoxymethyl side chain have been investigated. The activity against hepatitis B virus (HBV) has been tested.     

NMR Study on Fluoroisonucleosides( I)——Determination of the Configuration and Conformation of 1'''' -a-Methoxy-2'''' -Deoxy-2'''' -B-Ruoro-2'''' -a-Uracil -3'''' ,4'''' -o-lsopropylidene-L-Arabinoside

The present paper reports the determination of the configuration and Conformation of 1' -a-methoxy-2' -deoxy-2'-β-fluoro-2'-α-uracil-3',4' -o-isopropylidene-L-arabinoside obtained from silylated uracil by using 13C-NMR and 2D-NMR.     

Structure of Ethanol Coordinated 1,8,15,22-Tetra-(2'''',2'''',4''''-trimethyl-3''''-pentoxy)phthalocyaninatocobalt

1 INTRODUCTION Phthalocyanine and their metal complexes are important materials for the application in advanced technologies[1]. To meet some special purposes in various applications, the introduction of certain kind of substituents to the peripheral po…     

Synthesis of CF3-containing β-hetaryl-substituted enones

A procedure was developed for the synthesis of previously unknown CF₃-containing -azolyl-substituted enones by the reactions of 1,1,1-trifluoro-4-sulfonyl-3-butene-2,2-diols with various azoles. Quaternization of the azolyl group with methyl triflate afforded -azolium-substituted enones in quantitative yields.     

First Synthesis of 3''''- Geranyl-2'''', 3,4,4''''-tetrahydroxychalcone with 5 α- Reductase Inhibitory Properties

The geranylated chalcone 1,3′-geranyl-2′, 3,4,4′-tetvahydroxychalcone with high 5α-reductase inhibitory prop erties, was isolated from Artocarpus incisus by Shimizu in 2000. [1] Herein, we describe the first synthesis of the natural product 1 by four steps starting from compounds 2 and 7. The synthetic route was shown in Scheme 1:     

Synthesis and properties of β,β-sp3-hybridized subphthalocyanine analogues

A β,β-sp(3)-hybridized subphthalocyanine analogue, dibenzosubtriazachlorin, was synthesized, and its significantly split Q band absorptions in longer and shorter wavelength regions relative to those of subphthalocyanines were revealed. The effect of benzo-annulation to a subtriazachlorin structure on the position of the split Q bands as well as the electronic structures was also investigated.     

Syntheses of Novel 3-Substituted-2′-deoxy-3-deazauridine Nucleosides

Syntheses of novel 3-ethynyl (8), 3-vinyl (10) and 3-acetoxy (13)-2′-deoxy-3-deazauridine analogs starting from the protected 2′-deoxy-3-deazauridine derivative 4 are described.     

Synthesis and Novel Properties of Alkyl Thiphosporamidate Derivatives of Nucleosides

Novel alkyl thiophosphoramidate derivatives of nucleosde analogues(5) have been prepared by phosphochloridothioate chemistry.O-Isopropyl 2‘,3‘-O-isopropylidene uridine-5‘-yl N-thiophosphoryl threonine and serine methyl esters(5a and 5b )underwent the intramolecular catalyzed hydrolysis reaction.     

Synthesis and Novel Properties of Alkyl Thiophosphoramidate Derivatives of Nucleosides

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Facile Synthesis of 2-Fluorobenzofurans: 5-endo-trig Cyclization of β,β-Difluoro-o-hydroxystyrenes

Efficient synthetic methods were established for obtaining 2-fluorobenzofurans involving various substituents. Upon being treated with 1,8-diazabicyclo[5.4.0]undec-7-ene under microwave irradiation, the α-unsubstituted β,β-difluoro-o-hydroxystyrenes underwent nucleophilic 5-endo-trig cyclization to afford the corresponding 2-fluorobenzofurans in high yields. Furthermore, 2-fluoro-3-iodobenzofuran was successfully synthesized, and its transformation to various 3-substituted 2-fluorobenzofurans was demonstrated.     

Highly Efficient One-Pot,Three-Component Synthesis of β-Aminoketones Catalyzed by Fe(O2CCF3)3

A highly efficient one-pot, three-component synthesis of β-aminoketones was demonstrated using the cost-effective, noncorrosive, and easily available Fe(O₂CCF₃)₃ as a catalyst for the first time. The method can be employed to synthesize a wide range of target compounds and to introduce different functional groups into the β-aminoketone skeleton. Additionally, the method consistently has the advantages of good yields, short reaction time, and simply experimental workup procedure, which makes it a useful process for the synthesis of functionalized β-aminoketones.     

Synthesis of Unsymmetrical β-Arylaminoketones

Azomethines derived from aniline were condensed with acetophenone derivatives to obtain new unsymmetrical -arylaminoketones.     

New Synthesis of β-Iodostyrenes

A general procedure for the synthesis of -iodostyrenes is proposed. Aromatic aldehyde and ketone hydrazones are converted into the corresponding -iodostyrenes by treatment with CHI₃ in the presence of a catalytic amount of CuCl.     

Synthesis of β-Stannyl Esters

A synthesis of β-stannyl esters from ester enolates and iodomethyl (tri-n-butyl) stannane (3) is described.