SYNTHESIS OF 1-SUBSTITUTED 1H-1,2,4-TRIAZOLE DERIVATIVES

ＳＹＮＴＨＥＳＩＳＯＦ１－ＳＵＢＳＴＩＴＵＴＥＤ１Ｈ－１，２，４－ＴＲＩＡＺＯＬＥＤＥＲＩＶＡＴＩＶＥＳ￥ＹａｎＮｉａｎＳＨＩ；ＹａｎｇＹＡＮＧ；ＪｉａｎＸｉｎＦＡＮＧａｎｄＷｅｎＳｈｕｏＬＵ（Ｉｎｓｔ．ｏｆＥｌｅｍｅｎｔｏ－ＯｒｇａｎｉｃＣｈｅｍ．...     

SYNTHESIS OF SOME NORTROPANE DERIVATIVES

Some novel nortropane derivatives represented by structure Ⅱ and Ⅲ weresynthesized and tested for their affinity for dopamine receptors.     

A NOVEL SYNTHESIS OF 3-PHENYL-1H-INDAZOLE DERIVATIVES

ＡＮＯＶＥＬＳＹＮＴＨＥＳＩＳＯＦ３－ＰＨＥＮＹＬ－１Ｈ－ＩＮＤＡＺＯＬＥＤＥＲＩＶＡＴＩＶＥＳＺｈｅｎＱｉＺＨＯＮＧ；ＹｕＺｈｕＱＵＩ；ＺｈｅｎｇＺＨＡＮＧ，ａｎｄＨｏｎｇＷｅｎＨｕＤｅｐａｒｔｍｅｎｔｏｆＣｈｅｍｉｓｔｒｙ．ｈａｎｊｉｎｇＵｎｉｖ...     

SYNTHESIS AND CHARACTERIZATION OF POLYMER DERIVATIVES OF cis-PLATINUM COMPLEXES

Cis-platinum complexes used as antitumor drugs were attached onto preformed polymers toreduce the toxicity. Either alternating copolymer of styrene and maleic anhydride (CPSMA) orpolyacrylic acid (PAA) is readily dissolved in alkaline solution. The cis-platinum complexes areeasily converted into water soluble species when treated by silver nitrate in water. The expectedproducts could be obtained when the two aqueous solutions were brought together. The productswere characterized by elementary analysis, IR and XPS. The polymer derivatives could exchangeligands with nucleophilic groups in biological environment and also exhibit antineoplastic activity.     

SYNTHESIS AND CHARACTERIZATION OF TITANOCENE POLYMER DERIVATIVES

Titanocene polymer derivatives with potential antitumor properties were synthesized by interfacial condensation. The preformed polymers used are PAA (polyacrylic acid), CPSMA (1:1 alternating copolymer of styrene and maleic anhydride) and DVEMA (1:2 copolymer of divinyl ether and maleic anhydride). The ratio of practical and theoretical titanium content is 73.6%, 92.2% and 86.2% for PAA, CPSMA and DVEMA polymer derivatives respectively. The IR spectra of the polymer derivatives possess the characteristic absorptions of titanocene. XPS (X-ray photoelectron spectroscopy) of O_(1s) and Ti_(2p3/2) supports the existence of Ti-O bonding.     

SYNTHESIS AND CHARACTERIZATION OF DVE-CO-MA DERIVATIVES OF CIS- PLATINUM COMPLEXES

Copolymer of divinyl ether and maleic anhydride (DVE-co-MA) derivatives of cis-platinum complexes were synthesized and characterized by elementary analysis, IR and XPS ( X-ray photoelectron spectroscopy). The behavior of the products in biological environment was also studied. UV-visible and fluorescence spectra show that these polymer derivatives are able to exchange ligands with selected nucleophilic groups in biological environment.     

A CONVENIENT SYNTHESIS OF S-ALKYL PHENYLTHIOPHOSPHONIC ACID DERIVATIVES

The chlorination of O,O-dialkyl phenylthiophosphonates withphosphorus oxychloride proceeds with isomerization to give S-alkyl phenyl-thiophosphonochloridates,which react further with various nucleophilesin the presence of base to obtain the title compounds.     

SYNTHESIS OF NEW ESTRONE DERIVATIVES OF AMINO ACIDS AND PEPTIDES

A series of estrone derivatives of amino acids and peptides haze beensynthesized by different coupling reagents and the binding affinity of deblocked derivativesto the estrogen receptor of rats uteri have been measured by a comptetive radiometric bind-ing assay.     

A NEW AND EFFICIENT SYNTHESIS OF 3-IODO DERIVATIVES OF FLAVONES, THIOFLAVONES AND THIOCHROMONES

The title compounds are prepared in good yields by iodination of the corresponding flavones, thioflavones and thiochromones respectively using I_2-CAN(ceric ammonium nitrate) system. The compounds thus prepared are potentially useful precursors for the synthesis of C-3 linked binuclear compounds.     

REACTION OF ORGAINIC-TELLURONIUM YLIDE XI.A FACILE SYNTHESIS OF DERIVATIVES OF BISCYCLOPROPANE

Some telluronium salts react easily with 1,4-bis(3-substitutedphenyl-3-oxo-1-propenyl)benzene and 1,5-disubstituted phenyl-1,4-pentadien-3-one to afford derivatives of biscyclopropanes in 61.8-88.8% yield.     

SYNTHESIS AND SEMIEMPIRICAL CALCULATIONS OF THIAZOLIDINONE AND IMIDAZOLIDINONE DERIVATIVES OF α-DIONES

The condensation reactions of α-diones with rhodanine and creatinine to give acenaphthylidene, isatylidene and thioisatylidene derivatives, which may act as potential bioactive compounds, are described. The synthesized compounds have been characterized by elemental analysis and spectral studies, as well as by molecular modelling using PCWIN model.     

SYNTHESIS AND BIOLOGICAL ACTIVITY OF N-AROYL-N′-SUBSTITUTED THIOUREA DERIVATIVES

A series of N-aroyl-N′-substituted thiourea derivatives have been prepared in good to excellent yields under the condition of solid-liquid phase transfer catalysis using polyethylene glycol-400(PEG-400) as the catalyst. The products have been characterized on the basis of analytical and spectral (IR and ¹H NMR) data. The promoting effects of some compounds on wheat growth have been tested preliminary.     

SYNTHESIS OF 4,6-DISUBSTITUTED 5-THIOXO-1,2,4-TRIAZIN-3-ONE FROM BENZOTHIOFORMANILIDE

A method of synthesis of 4,6-disubstituted 5-thioxo-1,2,4-triazin-3-ones from benzothioformanilides and semicarbazide is described.And six newcompounds were synthesized by this method.     

AN EFFICIENT SYNTHESIS OF α-(BENZOTHIAZOL-2-YLOXY)PHOSPHONATES DERIVATIVES

Fifteen title compounds 3a-0 were synthesized by condensationof 2chloro-benzothiazole with a-hydroxyphosphonates in good yields us-ing potassium iodide/tetrabutyl ammonium bromide as catalyst.All new com-pounds have been identified by ~1H-NMR,IR and elemental analysis.     

SYNTHESIS AND ANTI－LIPID PEROXIDATION ACTIVITY OF AMINO ACID DERIVATIVES OF EBSELEN

ＳＹＮＴＨＥＳＩＳＡＮＤＡＮＴＩ－ＬＩＰＩＤＰＥＲＯＸＩＤＡＴＩＯＮＡＣＴＩＶＩＴＹＯＦＡＭＩＮＯＡＣＩＤＤＥＲＩＶＡＴＩＶＥＳＯＦＥＢＳＥＬＥＮ￥ＹｉａｇＸｉａＸＩＡＯ；ＸｉｕＦａｎｇＬＩＵ；ＨａｎＳｈｅｎｇＸＵ（ＤｅｐａｒｔｍｅｎｔｏｆＣｈｅｍｉ...     

SYNTHESIS OF 3-O-ARABINOSYLATED (1→6)-β-D-GALACTAN EPITOPES

Two tetrameric arabinogalactans, β-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl-(1→6)-[α-L-arabinofuranosyl-(1→3)]-D-galactopyranose (14) and α-L-arabinofuranosyl-(1→3)-β-D-galactopyranosyl-(1→6)-β-D-galactopyranosyl-(1→6)-D-galactopyranose (25), which are good candidates for CCRC-M7 epitope characterization, were synthesized efficiently using a convergent strategy. Migration of an acceptor acetyl group proved to be an obstacle to synthesis, but regioselective glycosylation or 4-O-benzyl protection of the acceptor circumvented this problem allowing efficient synthesis of the 1→6 linked target compounds.     

STUDIES ON THE SYNTHESIS AND ANTITUMOR ACTIVITY OF AMINO ACID ESTER DERIVATIVES OF BENZISOSELENAZOLONE

This paper reports a simple method for the synthesis of amino acid ester derivatives of benzisoselenazolone.Their anticancer activity is also given.These pharmaeological effeetshave been attributed to glutathione per     

SYNTHESIS OF ENANTIOMERICALLY ENRICHED α-AMINOPHOSPHINIC ACID DERIVATIVES VIA ASYMMETRIC HYDROGENATION

Abstract

For the first time, the biological interesting enantiomerically enriched α-aminophosphinic acids and their derivatives were prepared by asymmetric hydrogenation of suitable precursors and saponification of the obtained products. Enantiomeric excesses of up to 99 % were obtained.