Synthesis and Antibacterial Activities of 4—Amino—3—（1—aryl—5—methyl—1,2,3—triazol—4—yl）—5—mercapto—1,2,4—triazoles／2—Amino—5—（1—aryl—5—methyl—1,2,3—triazol—4—yl）—1,3,4—

Treatment of 4-amino-3-(1-aryl-5-methyl-1,2,3-triazol-4-yl)-5-mercapto-1,2,4-triazoles/2-amino-5-(1-aryl-5-methyl-1,2,3-triazole-4-yl)-1,3,4-thiadiazoles with benzaldehyde,acetone and ω-bromoacetophenone was tested and compared.The title compounds Schiff bases,amides,imidazolo [2,1-b]-1,3,4-thiadiazoles and 7H-s-triazolo[3,4-b]-1,3,4-thiadiazines have been confirmed by elemental analyses,^1H NMR,IR and MS spectra.All the compounds have also been screened for their antibacterial activities against B.subtilis,S.aureus and E.coli.     

Crystal and Molecular Structure of N—Phenyl 1—Methoxycarbonylmethyl—3—benzyl—1,2,3,4—tetrahydro—4—oxo—1,3,2—benzodiazaphosphorin—2—thiocarboxamide 2—Oxide

1 INTRODUCTIONOrganophosphorus compounds are ubiquitous in nature and they have broad applications in the fields of agriculture and medicine. During the past two decades, (-ketophosphonates and their derivatives containing sulfur have attracted considerable attention because these compounds are endowed with special physical, chemical and pharmacological properties due to the proximity of the carbonyl and the phosphoryl groups[1～8]. In the study on new pharmacenticals and agrochemicals, th…     

Synthesis and Crystal Structure of N—tert—butyl—N′—（2，4—dichlorobenzoyl）—N—[1—（4—chlorophenyl）—1,4—dihydro—6—methylpyridazine—4—oxo—3—carbonyl]hydrazine

1 INTRODUCTIONPyridazinone derivatives represent one of the most active classes of compounds possessing a wide spectra of biological activity. They are widely used in pharmaceuticals and agrochemicals[1,2]. Rohm- Haas Company had reported that N-tert-butyl- dibenzoylhydrazine exhibits excellent insecti- cides[3, 4] and t-butyl plays an important role in the insecticide activity [5]. In the previous paper, we had reported that 1-aryl-1,4-dihydro-3- acylhydrazino- carbonyl-4-one-6-methylpy…     

SYNTHESIS AND MOLECULAR STRUCTURE OF METHYL 1—BENZYL—6—PHENYLPIPERIDIN—2—ONE—5—CARBOXYLATE

<正> C20H21NO3,Mr=323.39,monoclinic, space group P21, a= 7. 338(2), b=15. 419(3),c=7. 515(1)A,β=95.98(1)°,V= 845. 7(2)A3,Dm(flotation in aq. KL)=1.267,Dx(Z=2)=1.270gcm-3,λ(MoKα)=0.71069A,μ=0.08cm-1,F(000)=344,T=295°K,final RF=0. 042 for 1651 observed reflections. The title compound was synthesized and established as the trans isomer, with the phenyl and carbomethoxy substituents occupying pseudo-axial and axial positions, respectively, of the piperidin-2-one ring in a half-chair conformation.     

Crystal Structure of 4—（4—chlorophenyl）—7,7—dimethyl—2,5—dioxo—1,2,3,4,5,6,7,8—octahydroquinoline

1 INTRODUCTION Since the discovery of the pharmacological effects of 1,4-dihydropridines(1,4-DHPs) as calcium channel blocks[1], a great deal of work has been directed towards synthesis of the novel 1,4-DHPs acting as calcium antagonists[2, 3]. In fact, it is well-established that slightly modified structures on the DHP exhibit a calcium agents effect[4, 5] ; however, two fused rings have been less well-studied. By refluxing equivalent amounts of dimedone, aromatic aldehyde Meldrum抯 …     

A New Solution—phase Parallel Synthesis of 2—Alkyamino—3—aryl—5—phenylmethylene—3,5—dihydro—4H—imidazol—4—ones

Thirteen new 2-alkylaminoimidazolones(4) wre rapidly synthesized by a new solution-phase parallel synthetic method,which includes aza-Wittig reaction of iminophosphorane(1) with aromatic isocyanate to give carbodi-imide(2) and subsequent reaction of 2 with various aliphatic primary amine in a parallel fashion.The products were confirmed by ^1H NMR,MS,IR and X-ray crystallographic analysis.The unusual selectivity of the cyclization was probably due to the deometry of the guanidine intermediate.     

On the Mechanism of Condensation between 5—Amino—4,6—dichloro—2—methylpyrimidine and 1—Acetyl—2—imidazolin—2—one

The condensation reaction between 5-amino-4,6-dichloro-2-methylprimidine and 1-acetyl-2-imidazolin-2-one using POCl3 as solvent gave 4,6-dichloro-2-methyl-5-(1-acetyl-tetra-hydro-imidazo-2-ylidene)-aminopyrimidine predominantly and 4,6-dichloro-2-methyl-5-{1-1-(2-oxo-tetrahydro-imidazolyl)]-acetene}-aminopyrimidine as by-product. No 4,6-dichloro-2-methyl-5-(1-acetyl-2-imidazolin-2-yl)-aminopyrimidine was found. The result indicated an esterifi-cation-addition-elimination mechanism.     

Michael Addition Reaction without Catalyst：The Synthesis of 2—Amino—5,6,7,8—tetrahydro—5—oxo—4—aryl—7,7—dimethyl—4H—benzo—[b]—pyran Derivatives

A serices of tetrahydrobenzo-[b]-pyran derivative was synthesized by the reaction of arylmethylene malononitrile or arylmethylene cyanoacetate with dimedone in ethylene gylcol at 80℃ without catalyst. The structures of the two products were characterized by X-ray diffraction.     

Synthesis of 3—Biaryl—1—ferrocenyl—2—propene—1—ones

The novel structures of organometallic compounds 3-biaryl-1-ferrocenyl-2-propene-1-ones 5 were synthesized for nonlinear optical chromophores by Suzuki cross-coupling reaction.Their structures were determined with elemental analyses,^1H NMR spectra and ^13C NMR spectra.