Synthesis of Novel 1-Arylsulfonyl-4-(1′-N-2′, 3′, 4′, 6′-tetra-O-acetyl-β-D-glucopyranosyl)thiosemicarbazides

Some 1-arylsulfonylthiosemicarbazides have been reported as fungicides1 and bacterio-static agents2. Recently, it is well documented that thiosemicarbazide is a novel class ofnon-peptide antagonists for bradykinin B2 , which is beneficial in the symptomat…     

N-取代-N′-(2′,3′,4′,6′-四-O-乙酰基-β-D-吡喃葡萄糖基）（酰）氨基硫脲的合成

利用2,3,4,6-四-0-乙酰基-β-D-吡喃葡萄糖异硫氰酸酯(I)分别和芳酰肼(Ⅱ),2-氨基-5-烷基/芳基-1,3,4-噻二唑(Ⅲ),3-烷基/芳基-4-氨基-5-巯基-1,2,4-三唑(Ⅳ),O,O-二烷基(硫代)磷酰肼(V,Ⅵ)反应,制得了目标物1a～1c,2d～2e,3f～3i,4j～4k和51等12种新化合物,IR,1H NMR和MS分析结果证明产物为β构型.     

Synthesis of N-Aryl-2- （1＇, 6＇-dihydro-6＇-pyridazinone-3＇-carbonyl） Thiosemicarbazides and Their Related Heterocyclic Compounds

1,6-Dihydro-3-hydrozinocarbonyl-6-pyridazinone (compound 2) were prepared from α-ketoglutaric acid and hydrazine hydrate. A series of N-aryl-2-(1‘,6‘-dihydro-6‘-pyridazinone-3‘-carbonyl) thiosemicarbazides 3a-3f were synthesized from the reaction of aryl isothiocyanates with compound 2. The terminal compounds 1,3, 4-thiadiazole, 1,3,4-oxadiazole and 1,2, 4-triazol-5-thione derivatives were cyclized from compounds 3a-3f. Their structures were confirmed by IR,^1H NMR, MS and elemental analyses.     

N-取代-N'-(2', 3', 4', 6'-四-O-乙酰基-β-D-吡喃葡萄糖基) (酰)氨基硫脲 的合成

利用2,3,4,6-四-O-乙酰基-β-D-吡喃葡萄糖异硫氰酸酯(Ⅰ)分别和芳酰肼(Ⅱ),2-氨基-5-烷基/芳基-1,3,4-噻二唑(Ⅲ),3-烷基/芳基-4-氨基-5-巯基-1,2,4-三唑(Ⅳ),O,O-二烷基(硫代)磷酰肼(Ⅴ,Ⅵ)反应,制得了目标物1a～1c,2d～2e,3f～3i,4j～4k和5l等12种新化合物,IR,^1HNMR和MS分析结果证明产物为β构型。     

1-芳酰基-4-(1＇-N-β-D-吡喃型糖基)氨基硫脲类化合物的合成

通过2,3,4,6-四-O-乙酰基-β-D-吡喃型葡萄糖异硫氰酸酯和2,3,4-三-O-乙酰基-β-D-吡喃型木糖异硫氰酸酯与取代的芳基酰肼的亲核加成反应合成了10个1-芳酰基-4-(1＇-N-2＇,3＇,4＇,6＇-四-O-乙酰基-β-D-吡喃型葡萄糖基)氨基硫脲和7个1-芳酰基-4-(1＇-N-2＇,3＇,4＇-三-O-乙酰基-β-D-吡喃型木糖基)氨基硫脲,所得化合物的结构经元素分析,IR,1H NMR确证.     

Synthesis and Characterization of N-（ 2,3,4,6-Tetra-O-acetyl-β-D-glucopyranosyl） -thiocarbamic-4-hydroxy-benzoyl Hydrazine Dihydrate

Introduction The studies on carbohydrate-containing compoundshave extremely been increased during the last threedecades because these compounds have many interest-ing and useful biological activities besides structuralsupport and energy storing functions[1]. Many nomadicsugars play an important role in biology[2]and many bi-ologically important products have a sugar unit connect-ed with the main structures by means of an atom(O, S,N or C) or a group of atoms[3]. Alarge number of con-formatio…     

Synthesis and Biological Activity of Novel 2,3-Dihydro-2-phenylsulfonylhydrazono-3-(2′,3′,4′,6′-tetra-O-acetyl-β-D-glucopyranosyl)thiazoles

A series of novel 2,3-dihydro-2-phenylsulfonylhydrazono-3-(2',3',4',6'-tetra-O-acetyl-β-D-glucopyranosyl) thiazoles were designed and synthesized via the reaction of thiosemicarbazide with chloroaldehyde.Their chemical structures were characterized by 1H and 13C NMR spectroscopy and elemental analysis.The bioassay results indicate that some of these compounds exhibit moderate fungicidal and herbicidal activities.     

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.     

Synthesis and Molecular Structure of 1,5,1 ＇,5 ＇-Tetraphenyl- 1H, 1H ＇-3,3 ＇- dialkylthio-bi- 1,2,4-t riazole

The title compound 1,5,1',5'-tetraphenyl-1H,1H'-3,3'-dialkylthio-bi-1,2,4-tri- azole (2, C28H20N6S2, Mr = 504.62) was prepared by the reaction of 1-benzoyl-3-phenylamino- thiourea 1 and Mn(OAc)3·2H2O in acetic acid under microwave irradiation. The crystal is of monoclinic, space group P21/c with a = 11.3931(10), b = 16.5787(14), c = 26.470(2) , β = 98.274(2)o, Z = 8, V = 4947.8(8) 3, Dc = 1.355 g/cm3, μ(MoKα) = 0.245 mm-1, F(000) = 2096, the final R = 0.0583 and wR = 0.1502 for 8705 observed reflections (I > 2σ(I)). X-ray analysis reveals that the title compound is 1,5,1',5'-tetraphenyl-1H,1H'-3,3'-dialkylthio-bi-1,2,4-triazo- le, and its formation mechanism was proposed.     

1—芳酰基—4—（1‘—N—β—D—吡喃型糖基）氨基硫脲类化合物的合成

通过２,３,４,６－甲－Ｏ－乙酰基－β－Ｄ－吡喃型葡萄糖异硫氰酸酯和２,３,４－三－Ｏ－乙酰基－β－Ｄ－吡喃型木糖异硫氰酸酯与取代的芳基酰肼和亲核加成反应合成了１０个１－芳酰基－４－（１’－Ｎ－２’,３’,４’,６’－四－Ｏ－乙酰基－β－Ｄ－吡喃型葡萄糖基）氨基硫脲和７个１－芳酰基－４－（１’－Ｎ－２’,３’,４’－三－Ｏ－乙酰基－β－Ｄ－吡喃型木糖基）氨基硫脲,所得化合物的结构经元素分析,ＩＲ,     

Synthesis and Anti-HIV Activity of Trisubstituted （3＇R, 4＇R）-3＇,4＇-Di-O-（S）-camphanoyl-（＋）-c/s-khenactone （DCK） Analogs

To further explore the potential of DCK analogs as anti-HIV drug candidates, ten new tri-substituted （3＇R,4＇R）-3＇,4＇-di-O-（S）-camphanoyl-（＋）-cis-khellactone （DCK） derivatives （4-13） were designed, synthesized, and evaluated against HIV replication in MT4 cells and H9 lympho- cytes.     

Synthesis and Crystal Structure of 1＇-Methyl-4＇-（4-chlorophenyl）-1H-indole-3-spiro-2＇-pyrrolidine-3＇-spiro-4＂-（2＂-phenyloxazole）-2,5＂（3H,4＂H）-dione

The title compound （C26H20ClN3O3） has been synthesized by 1,3-dipolar cycloaddition reaction from isatin, sarcosine and （Z）-4-（4-chlorobenzylidene）-2-phenyloxazol-5（4H）-one through a one-pot procedure, and its structure was confirmed by IR, IH NMR, elemental analysis and single-crystal X-ray diffraction analysis. The crystal belongs to the triclinic system, space group PI, with a = 9.3903（19）, b = 11.398（2）, c = 12.603（3） A, α = 83.495（3）, β = 68.988（3）, γ = 67.178（3）^o, V= 1160.1（4）A^3 Z = 2, Mr= 457.90, Dc= 1.311 g/cm^3, p = 0.198 mm ^-1, F（000） = 476, the final R = 0.0489 and wR = 0.1144 for 3109 observed reflections with I 〉 2σ（I）.     

Synthesis of Conformationally Locked 2＇-Deoxy-2＇-nucleobase-5＇- Isonucleosides: 2＇-Deoxy-2＇-nucleobase-5＇ deoxy-1＇, 4＇ :3＇, 6＇-dianhydro-D-mannitol

Novel bicyclic isonucleosides, 2＇ -deoxy- 2＇ -nucleobase- 5＇ -deoxy- 1＇ , 4＇ : 3＇ , 6＇ -dianhydro D-mannitol 10a-10c, were synthesized from D-glucose. The computer-assisted molecular simu lation indicated that the sugar conformations of compounds 10a-10c were restricted to N-con formation.     

Synthesis of Novel 1-Alkyl-2-chloro（alkoxy）-1H-indole 3-Carbaldehyde Oximes and Oxime-ethers（esters） Derivatives

A convenient synthesis of 1-alkyl-2-chloro-1H-indole-3-carbaldehyde oximes(5a―5d) and 1-alkyl-2-phenoxy-1H-indole-3-carbaldehyde oximes(6a―6d) from 2-indolone was completed via the Vilsmeier-Haack reac-tion,with N-alkylation and oximation as the key steps.An improved one-pot method for the synthesis of 1-alkyl-2-alkoxy-1H-indole-3-carbaldehyde oximes(7a―7h) from 1-alkyl-2-chloro-1H-indole-3-carbaldehydes(3a―3d) was described.The Williamson reactions and esterification reactions were performed and the oxime-...     

Synthesis and Crystal Structure of 4-（2-Methylene-1-ethyl-3,3-dimethylindoline-2＇-yl）-6,8-dibromo-1＇-ethyl-3＇,3＇-dimethylspiro-[3,4-dihydro-2H-1-benzopyran-2,2＇-indoline]

The title compound of 4-(2-methylene-1-ethyl-3,3-dimethylindoline-2'-yl)-6,8-dibro-mo-1'-ethyl-3',3'-dimethylspiro[3,4-dihydro-2H-1-benzopyran-2,2'-indoline],C33H36Br2N2O,as a dicondensed spiropyran(DC) has been synthesized by indoline in ethanol with 3,5-dibromo-salicyaldehyde.The compound was characterized by elemental analysis and IR spectra.Meanwhile,the crystal of the compound was obtained and determined by X-ray single-crystal diffraction.Crystal data:monoclinic system,space group P21/n,a=12.9699(15),b=12.5196(13),c=19.327(2),β=106.493(3)°,Mr=636.46,V=3009.1(6) 3,Z=4,F(000)=1304,Dc=1.405 g/cm3,μ=2.722 mm-1,R=0.0554 and wR=0.1176 for 6892 independent reflections(Rint=0.0354) and 5699 observed reflections(Ⅰ 2σ(Ⅰ)).     

Synthesis and Crystal Structure of 2-tert-Butyl-5-（4-tert-butylbenzylthio）- 4-chloropyridazin-3 （2H） -one

IntroductionPyridazinone compounds show widespread biologi-cal activities[1—3], many of them have been developedand used as fungicides and acaricides[4,5]. Pyridaben isa novel pyridazinone derivative that shows acaricide andinsecticide properties and was…