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 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.     

STUDIES ON THE SYNTHESIS AND BIOLOGICAL ACTIVITY OF 1-ARYLOXYACETYL-4-AROYLTHIOSEMICARBAZIDE DERIVATIVES

A series of new 1-aryloxyacetyl-4-aroylthiosemicarbazides were synthesized by means of solid-liguid phase transfer catalysis. The promoting effects of these new compounds on wheat growth were observed.     

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

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

STUDIES ON THE SYNTHESIS OF ISOSARCOPHYTOL-A

A precursor 9 of isosarcophytol-A(1)was prepared from(■)-farnesol(3)through 6 steps.Isosarcophytol-A(1),a cembrane-type diterpenoid,was first isolated fromustralian soft coral(Nephthea brassica)in 1982,and its structure was estab-shed as(1,3,7,11-all ■,13■)-cembra-1,3,7,11-tetraen-13-ol,an isomer ofarcophytol-A■.As far as we know,its bioactivity and synthesis have noteen reported yet.     

STUDIES ON THE STEREOSELECTIVITY AND SUBSTITUTED GROUPS OF (+)-CAMPHOR DERIVATIVES

From (+)- camphor, six new (+)-camphor derivatives were synthesized. According tothe structure and chemical properties of the derivatives, the relation between the substitutedgroups and the stereoselectivity of alkylations and reduction was examined. It is found thatthe chemical shift of protons of C(8), C(9) methyl groups and chemical properties of carbonylO(2) are associated with the substituted groups.     

STUDIES ON CHIRAL THIOPHOSPHORIC ACIDS AND THEIR DERIVATIVES [ⅤⅢ]——THE STEREOCHEMISTRY OF SOME REACTIONS OF THE MIXED ANHYDRIDE OF O-ETHYL PHENYLPHOSPHONOTHIOIC AND O-ETHYL O-PHENYL PHOSPHOROTHIOIC ACIDS

In this paper, (1) alkaline methanolysis, (2) acid methanolysis, (3) alkaline hydro-lysis, (4) aminolysis of (+)-(R)-(R)-mixed anhydride 1 of O-ethyl phenylphosphonothioic:and O-ethyl O-phenylphosphorothioic acid, (5) its reactions with KSH and (6) with PCl_5have been studied. The cleavage of P-O-P bonds in all the reactions studied has beenfound. In reactions (1)-(4), attacks of nucleophiles occur to the phosphorus atoms of phos-phonyl groups forming the products with inversion of configuration, while the configurationof the phosphorus atoms of phosphoryl groups which are not attacked is retained. Inreaction (5), the uncleophile -SH attacks the phosphorus atom of the phosphonyl group,but a racemic product results because of the formation of ph(EtO)P(S)~- which loseschirality; the configuration of the phosphorus atom of the phosphoryl group which is notattacked is still retained. In reaction (6), both the phosphonyl and phosphoryl groups arechlorinated giving as products (-)-(R)-thiophophonyl chloride 1     

STUDIES ON THE LOW-TEMPERATURE SYNTHESIS OF METHANOL BY CARBONYLATION AND HYDROGENOLYSIS

The present process may be less energy intensive compared withthe existing processes.A proprietary amide aleohol additive can markedly in-hibit the deactivation of CH_3ONa catalyst for methanol carbonylation.Thespace-time yield(STY)of the methyl formate(MF)is 625g·1 ~1h ~1after 40htime on stream with theadditive,while the yield is only 190g·1 ~1h ~1without the additive at the same reaction conditions.By using four types of tubu-lar reactors without any mechanico-rotary parts and hige speed circulation ofthe reactants for the carbonylation at P_(CO)=5MPa,a 95% single pass conversion of CO and 645g·1 ~1h ~1of STY of MF were obtained.A novel Cu-ZnO/Al_2O_3 catalyst for MF hydrogenolysis to methanol is reported in this pa-per.The Cu-ZnO/Al_2O_3 catalyst is characterized by the resistance to poison-ing of high concentration CO up to 16.2v%.     

STUDIES ON THE SYNTHESIS AND DNA-BINDING ABILITY OF ZINC FINGER MOTIF

ＳＴＵＤＩＥＳＯＮＴＨＥＳＹＮＴＨＥＳＩＳＡＮＤＤＮＡ－ＢＩＮＤＩＮＧＡＢＩＬＩＴＹＯＦＺＩＮＣＦＩＮＧＥＲＭＯＴＩＦ￥ＸｉａｏＹｕＨＵ；ＲｕｉＷＡＮＧ；ＸｉａｎｇＱｕｎＬＩ（ＳｔａｔｅＫｅｙＬａｂｏｒａｔｏｒｙｏｆＡｐｐｌｉｅｄＯｒｇａｎｉｃＣｈｅ...     

SYNTHESIS OF SULFOXIDES AND THEIR STRUCTURE-REACTIVITY STUDIES ON THE LANTHANIDE EXTRACTION

Modified methods for the synthesis of various sulfoxides with isomeric octyl groups, i.e.dioetyl sulfoxides, bis (octylsulfenyl) methane and bis (octylsulfenyl) ethane are described. Theextraction behaviours of these sulfoxides for lanthanides from nitric acid system are studiedand discussed on the basis of their chemical structures. The composition and the structureof the extracted species are deduced by method of continuous variation as well as by ele-mental and thermo-gravimetric analysis. As shown by infrared spectroseopic studies thesulfenyl oxygen acts as coordinating atom and the NO_3 serves as bidentate.     

STUDIES ON THE SYNTHESIS OF SINULARIOE-D,SINULARIAL-A AND SINULARIC ACID-A

A precursor 12 of sinulariol-D,sinularial-A and sinularic acid-A(marinecembranoids)was prepared from geraniol through nine steps     

PEPTIDE SELF－FORMATION FROM N－DIISOPROPYLOXY PHOSPHORYL AMINO ACIDS AND PREBIOTIC SYNTHESIS OF PROTEIN

ＰＥＰＴＩＤＥＳＥＬＦ－ＦＯＲＭＡＴＩＯＮＦＲＯＭＮ－ＤＩＩＳＯＰＲＯＰＹＬＯＸＹＰＨＯＳＰＨＯＲＹＬＡＭＩＮＯＡＣＩＤＳＡＮＤＰＲＥＢＩＯＴＩＣＳＹＮＴＨＥＳＩＳＯＦＰＲＯＴＥＩＮ￥ＹｏｎｇＪＵ；ＹｉＣＨＥＮａｎｄＹｕＦｅｎＺＨＡＯ（Ｂｉｏｏｒｇａ...     

STUDIES ON THE PRENYLFLAVONOIDS PART Ⅹ：THE TOTAL SYNTHESIS OF ANTIARONE－C AND ANTIARONE－H

ＳＴＵＤＩＥＳＯＮＴＨＥＰＲＥＮＹＬＦＬＡＶＯＮＯＩＤＳＰＡＲＴⅩ：ＴＨＥＴＯＴＡＬＳＹＮＴＨＥＳＩＳＯＦＡＮＴＩＡＲＯＮＥ－ＣＡＮＤＡＮＴＩＡＲＯＮＥ－ＨＹｕＬｉｎＬＩ；ＬｉａｎＹｅＺＨＡＯ（ＳｔａｔｅＫｅｙＬａｂｏｒａｔｏｒｙｏｆＡｐｐｌｉｅｄＯ...     

THE ASYMMETRIC SYNTHESIS OF AMINO ACIDS UNDER POLYMER-SUPPORTED PHASE TRANSFER CATALYTIC CONDITION

The optical α-amino acids were synthesized under room temperature byalkylation of N-(diphenyl methylene) glycine t-butyl ester under polymer-supported phasetransfer conditions using polymer-supported cinchonine (or quinine) alkaloids as chiralphase transfer catalysts and dichloromethane as solvent, followed by hydrolysis of theabove intermediates introduced to the final products-optical α-amino acids. This is anew method for the asymmetric synthesis of α-amino acids. The influences of catalyst,temperature, substrates, and organic solvents on the chemical yield and optical purities ofproducts were studied.     

STUDIES ON CHIRAL THIOPHOSPHORIC ACIDS AND THEIR DERIVATIVES 13．THE ASYMMETRIC CYCLIZATION OF （＋）－SUBSTITUTED CYCLOPENTANODIAMINE WITH O－ARYL THIOPHOSPHOROCHLORIDATES

ＳＴＵＤＩＥＳＯＮＣＨＩＲＡＬＴＨＩＯＰＨＯＳＰＨＯＲＩＣＡＣＩＤＳＡＮＤＴＨＥＩＲＤＥＲＩＶＡＴＩＶＥＳ１３．ＴＨＥＡＳＹＭＭＥＴＲＩＣＣＹＣＬＩＺＡＴＩＯＮＯＦ（＋）－ＳＵＢＳＴＩＴＵＴＥＤＣＹＣＬＯＰＥＮＴＡＮＯＤＩＡＭＩＮＥＷＩＴＨＯ－ＡＲＹ...     

STUDIES ON 12－MOLYBDOVANADOPHOSPHORIC ACIDS APPLIED TO THE SELECTIVE OXIDATION OF ACROLEIN

ＳＴＵＤＩＥＳＯＮ１２－ＭＯＬＹＢＤＯＶＡＮＡＤＯＰＨＯＳＰＨＯＲＩＣＡＣＩＤＳＡＰＰＬＩＥＤＴＯＴＨＥＳＥＬＥＣＴＩＶＥＯＸＩＤＡＴＩＯＮＯＦＡＣＲＯＬＥＩＮ￥ＺｈｉＤｏｎｇＺＨＵ（ＤｅｐａｒｔｍｅｎｔｏｆＣｈｅｍｉｓｔｒｙ，ＳｕｚｈｏｕＵｎｉｖｅ...     

STUDIES ON CHIRAL THIOPHOSPHORIC ACIDS AND THEIR DERIVATIVES——STEREOCHEMISTRY OF ALKALINE HYDROLYSIS OF OPTICALLY ACTIVE O-ETHYL O-PHENYL PHOSPHOROTHIOIC DERIVATIVES

The reaction of optically active O-ethyl O-phenyl phosphorochloride 1 with alcohol, phenol,amine, mercaptan or thiophenol, respectively, in the presence of an alkali obtained optically activeO-ethyl O-phenyl phosphorothioic derivatives 2 with inversion of configuration. The hydrolysis of 2was carried out in 1 N NaOH-dioxane solution. The hydrolysis of 2a and 2h predominantly gaveproducts with inversion of configuration with OPh as leaving group, but also gave products withretention of configuration with OMe or SPr as leaving group. Exclusive products with inversion ofconfiguration with OPh as leaving group were only obtained from the hydrolysis of 2b, 2f and 2g.The hydrolysis of 2c gave product with inversion of configuration with OC_6H_4NO_2-p as leavinggroup. From 2d, 2e and 2i, products with retention of configuration were formed with OC (Me)-CHCO_2 Et(Z), OC(Me)-CHCO_2Et(E) and SPh as leaving group, respectively. All the above resultscan be satisfactorily interpreted in the light of trigonal bipyram     

STUDIES ON STRUCTURE AND SYNTHESIS OF ARTEANNUIN AND ITS RELATED COMPOUND Ⅴ——THE TOTAL SYNTHESIS OF ISODEOXYARTEANNUIN

The total synthesis of isodeoxyarteannuin 3 was achieved starting from norsesquiterpenoid lactone 5 which was obtained from 10-R( )-citronellal 4. The synthetic route is Summarized in Fig. 1.