Showing papers on "Pyrazole published in 1989"
Patent•
05 Jan 1989TL;DR: Substituted pyrroles, pyrazoles and triazoles such as and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure as discussed by the authors.
Abstract: Substituted pyrroles, pyrazoles and triazoles such as and their pharmaceutically suitable salts are useful as antihypertensive agents and for treatment of congestive heart failure.
150 citations
TL;DR: In this paper, the relationship between the structures of diverse heterocyclic nitrogen compounds and the effectiveness of these compounds for the inhibition of nitrification in soil was studied by determining the effects of different amounts of 12 unsubstituted and 33 substituted HN compounds.
Abstract: The relationship between the structures of diverse heterocyclic nitrogen (N) compounds and the effectiveness of these compounds for the inhibition of nitrification in soil was studied by determining the effects of different amounts of 12 unsubstituted and 33 substituted heterocyclic N compounds on the production of (NO
2
−
+NO
3
−
)-N in soils incubated at 25 °C for 21 days after treatment with ammonium sulfate. The results showed that unsubstituted heterocyclic N compounds containing two adjacent ring N atoms inhibit nitrification in soil and that two of these compounds, pyrazole and 1,2,4-triazole, are potent inhibitors. They also showed that several substituted pyrazoles and thiadiazoles are good inhibitors of nitrification in soil (e.g., 3-methylpyrazole and 3,4-dichloro-1,2,5-thiadiazole).
98 citations
TL;DR: In this article, the reaction of bis(pyrazolyl)propane (CH3)2C(pz)2, (pzH = pyrazole), with PtCl2, RCN2PtCl2 and K2[PtCL4 have been investigated, and the results compared with those described previously for the corresponding palladium(II) derivatives.
56 citations
TL;DR: In this article, 3-Amino-4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1 H -pyrazole 7aw was the most potent 7aw also had a potent inhibitory effect on cyclooxygenase and thromboxane synthetase and platelet aggregation.
49 citations
TL;DR: In this article, the inhibition of corrosion of commercial 67/33 brass in 0.1m HCl acid solutions by some amino pyrazole derivatives was tested using polarization, capacitance and weight-loss measurements.
Abstract: The inhibition of corrosion of commercial 67/33 brass in 0.1m HCl acid solutions by some amino pyrazole derivatives was tested using polarization, capacitance and weight-loss measurements. The amino pyrazole derivatives were 3(5)-amino, 5(3)-phenyl pyrazole; 3(5)-amino, 5(3)[4--chlorophenyl] pyrazole; 3(5)-amino, 5(3)[4--methoxy phenyl]pyrazole; 3(5)-amino, 5(3)[4--methyl phenyl]pyrazole; 3(5)-amino, 5(3)-cyano pyrazole; and 3(5)-amino, 4-phenyl-5(3)-methyl pyrazole. The results showed that these compounds predominate as cathodic inhibitors and inhibition efficiencies up to 91% can be obtained. The inhibition was assumed to occur via chemisorption of the inhibitor molecules fitting a Temkin isotherm. The influence of the substituent group on the inhibition efficiency of the inhibitor was explained in terms of the density of the electron cloud on the pyrazole ring and the mode of adsorption. Although increase in temperature was found to decrease the corrosion in the absence of the inhibition, it increased in the presence of inhibitor, probably via desorption of the inhibitor molecules.
45 citations
Patent•
29 Aug 1989
TL;DR: In this article, a (3-substituted phenyl)-pyrazole derivative represented by the general formula (I) wherein R1, R2, R3, R4 and X are various substituents and a salt thereof, and its production process is disclosed.
Abstract: OF THE DISCLOSURE There are disclosed a (3-substituted phenyl)-pyrazole derivative represented by the general formula (I) wherein R1, R2, R3, R4 and X are various substituents and a salt thereof, and its production process. Said pyrazole derivative or its salt is useful as a herbicide for controlling various injurious weeds.
39 citations
TL;DR: In this paper, the authors showed that 6-amino-5-cyano-4-aryl-2-methyl-4H-pyran-3-carboxylates 4 could be converted into 1,6-diazanaphthalene, pyrano-[2,3-c]pyrazole, isoxazolo[3,4-b]pyridine, Pyrano[2, 3-b]-polycyclic pyridine derivatives on treatment with malononitrile, hydrazine hydrate,
39 citations
Patent•
12 Oct 1989TL;DR: In this article, a novel pyrazole amide and an insecticidal and miticidal composition containing the amide as an active ingredient are described, which shows excellent insecticide and miticide activities.
Abstract: Novel pyrazole amide and an insecticidal and miticidal composition containing the pyrazole amide as an active ingredient are described. The pyrazole amide according to the present invention shows excellent insecticidal and miticidal activities.
38 citations
TL;DR: The corrosion inhibition of zinc in HCl solutions by several pyrazole derivatives was studied in this article, including 3(5) amino, 5(3) phenylpyrazole; 3( 5] amino, 3[4] [4] methylphenyl] pyrazide derivatives.
Abstract: The corrosion inhibition of zinc in HCl solutions by several pyrazole derivatives—namely, 3(5) amino, 5(3) phenylpyrazole; 3(5) amino, 5(3) [4′—methylphenyl] pyrazole; 3(5) amino, 5(3) [4′...
37 citations
TL;DR: In this article, the synthesis, spectroscopy and structure of mononuclear transition metal coordination compounds of the ligands tris(1-pyrazolylmethyl)amine (amtp) and bis(1 -pyrazylmethyl)amines (am2p) are described.
36 citations
TL;DR: In this paper, new dinucleating ligands containing pyrazole as an endogenous bridging group, 3,5-bis-[N-(2-pyridylmethyl)carbamoyl] pyrazoles (H3L1), 3, 5-bis{N-[2-(diethylamino)ethyl] carbamoyls}pyrazole (H 3L2), and 3, 2-dimethylamino)-propyl] carbamide-propyl]-polypropyl-carbamide-pyrazoles(H3
Abstract: New dinucleating ligands containing pyrazole as an endogenous bridging group, 3,5-bis-[N-(2-pyridylmethyl)carbamoyl] pyrazole (H3L1), 3,5-bis{N-[2-(diethylamino)ethyl]carbamoyl}pyrazole (H3L2), and 3,5-bis{N-[3-(dimethylamino)propyl]carbamoyl}pyrazole (H3L3), and their binuclear copper(II) complexes with azide or acetate ion as an exogenous bridge, [CU2L(N3)(H2O)2]·H2O(L = L1–L3) and [Cu2L1(O2CMe)]·2MeOH, have been obtained. Cryomagnetic investigations (5–300 K) reveal a significant antiferromagnetic spin exchange for the azide-bridged complexes(–J= 371–297 cm–1), but a ferromagnetic spin exchange (J > +8.9 cm–1) for the acetate-bridged complex. The azide-bridged complexes are e.s.r. silent. The acetate-bridged complex is unstable in dimethylformamide (dmf) but a quickly prepared dmf frozen solution of the sample gives X-band signals characteristic of a spin-triplet (S= 1) state, together with signals due to a spin doublet(S=½) attributable to monomeric copper(II). Signals at 812, 1 292, and 4 380 G show a seven-line hyperfine structure (Azz= 0.0103 cm–1); the first and third signals are assigned to ΔMs= 1 transitions and the second to the ΔMs= 2 transition of the parallel resonance of the spin-triplet state. E.s.r. simulation based on the spin Hamiltonian for the spin triplet of a dicopper(II) system gives gzz= 2.533, D= 0.210 cm–1, and E= 0.020 cm–1. Only two components of the perpendicular resonances are recognizable at 2 113 and 3 812 G which give gx= 2.055.
TL;DR: In this article, a method for the preparation of condensed pyranones is presented. But the method is not suitable for the extraction of condensed Pyranone derivatives, such as barbituric acid derivatives, pyrazolones and resorcinol.
TL;DR: In this paper, the synthesis of tricyclic compounds with an imidazole, triazole or tetrazole ring fused to the pyrazolo[3, 4-d]pyrimidine ring system, in an angular position (C-4 and N-5), was described.
Patent•
30 Aug 1989
TL;DR: In this paper, a (3-substituted phenyl)pyrazole derivative represented by the general formula ##STR1## was disclosed, wherein R1, R2, R3, R4 and X are various substituents and a salt thereof, and its production process.
Abstract: There are disclosed a (3-substituted phenyl)pyrazole derivative represented by the general formula ##STR1## wherein R1, R2, R3, R4 and X are various substituents and a salt thereof, and its production process. Said pyrazole derivative or its salt is useful as a herbicide for controlling various injurious weeds.
TL;DR: Although the compounds of the CGS series are potent ligands of the benzodiazepine receptors, none of the isosteres tested showed any significant inhibiting potency, which may be due to the change in electronic properties brought about by the replacement of the NH of theCGS series with an oxygen atom.
TL;DR: In this article, the preparation of facially coordinating tridentate ligands is described, which contain a phenol and either two imidazole, two pyridine or two pyrazole donor atoms.
TL;DR: Isomerization of the di-iridium(II) complex [Ir2(CO)2PPh3]2(µ-pz)2( µ-CH2)(I)2] has been found to be intramolecular by mass spectrometric analysis of isotope distribution (13C and 2H) in isotopomers of (7) formed from (2) containing 13CO or C2H2I groups or both, and the (2)-(7) conversion shows first-order behaviour which is conspicuously retarded by added
Abstract: Isomerization of the di-iridium(II) complex [Ir2(CO)2(PPh3)2(µ-pz)2(CH2I)(I)](2, Hpz = pyrazole) to the di-iridium(III) methylene complex [Ir2(CO)2(PPh3)2(µ-pz)2(µ-CH2)(I)2](7) which occurs on reflux in benzene solution has been found to be intramolecular by mass spectrometric analysis of isotope distribution (13C and 2H) in isotopomers of (7) formed from (2) containing 13CO or C2H2I groups or both, and the (2)–(7) conversion shows first-order behaviour which is conspicuously retarded by added PPh3; an X-ray crystal structure determination for compound (7) confirms that the two Ir centres lie outside bonding range at 3.432(1)A with tetrahedral µ-CH2.
TL;DR: Phenacylmalonononitriles 2 react with hydrazines, acetic-hydrochloric acid and with diazotised primary aromatic amines to afford phenacylpyrazole (5a,b), aminofurans (6a, b) and aminopyrazole derivatives (3a,d) respectively.
Abstract: Phenacylmalononitriles 2 react with hydrazines, acetic-hydrochloric acid and with diazotised primary aromatic amines to afford phenacylpyrazole (5a,b), aminofurans (6a,b) and aminopyrazole derivatives (3a,d) respectively. The synthesised derivatives (3d, 6a) were the key materials for the synthesis of isoindolinedione, (7a–c) pyrazolopyrimidine (9, 10), and pyrazolopyridazine derivatives (11). The structures of the newly synthesised heterocycles were established on the basis of elemental analyses and spectral data besides synthesis via other routes.
TL;DR: In this article, N-unsubstituted pyrazole derivatives were converted into 5-subtituted 1-lithioxymethyl pyrazoles in a one-pot sequence using formaldehyde both for N-protection and to mediate lithiation at the 5-position.
TL;DR: In this paper, the authors investigated the reaction of six π-rich N-heteroaromatic compounds (2-7) and five xanthine derivatives (8-12) in the presence of platinated palladium-carbon (Pd-Py/C) catalyst.
Abstract: Dimerization reactions of six π-rich N-heteroaromatic compounds (2-7) and five xanthine derivatives (8-12) in the presence of platinated palladium-carbon (Pd-Py/C) catalyst were investigated. N-Methylimidazole (2), benzimidazole (4) and N-methylbenzimidazole (5) condensed dehydrogenatively to afford the corresponding symmetric dimers when heated in the presence of Pd-Pt/C catalyst and pyridine N-oxide (1). On the other hand, imidazole (3), pyrazole (6) and N-methylpyrazole (7) did not dimerize under the same conditions. The same reactions using caffeine (10), 1, 7-dimethylhypoxanthine (9) gave the corresponding dimers.
Patent•
16 Jun 1989
TL;DR: Condensed pyrazole 3-oxo-propanenitrile derivatives of formula (I) have immunomodulating activity and can be used in particular as immunostimulating agents, e.g. in the treatment of acute and chronic infections of both bacterial and viral origin this article.
Abstract: Condensed pyrazole 3-oxo-propanenitrile derivatives of formula (I)
wherein X represents a - CH(R 4 .)-group, an oxygen atom or a - S(O) n group where n is 0, 1 or 2; R 1 represents C 1 -C 6 alkyl, pyridyl or unsubstituted or substituted phenyl; R 2 , R 3 and R 4 . are as defined herein; and Q represents hydrogen, carboxy, C 2 -C 7 alkoxycarbonyl or a - CON(R a )R b group, R a and R b being as defined herein; and their pharmaceutically acceptable salts have immunomodulating activity and can be used in particular as immunostimulating agents, e.g. in the treatment of acute and chronic infections of both bacterial and viral origin, alone or in association with antibiotic agents, and in the treatment of neoplastic diseases, alone or in association with antitumoral agents, in mammals.
Patent•
27 Feb 1989TL;DR: In this paper, a support for thermal dye transfer comprises a support having thereon a dye dispersed in a polymeric binder, the dye having the formula: ##STR1## wherein each R 1 independently represents hydrogen, a substituted or unsubstituted alkyl group having from 1 to about 10 carbon atoms; R 3 and R 4 each independently represents R 1, with the proviso that at least one of R 3, R 4 is hydrogen; R 5 represents hydrogen; halogen; cyano; and R 6 represents hydrogen.
Abstract: A yellow dye-donor element for thermal dye transfer comprises a support having thereon a dye dispersed in a polymeric binder, the dye having the formula: ##STR1## wherein each R 1 independently represents hydrogen, a substituted or unsubstituted alkyl group having from 1 to about 10 carbon atoms; a cycloalkyl group having from about 5 to about 7 carbon atoms or an aryl group having from about 6 to about 10 carbon atoms; R 2 represents a substituted or unsubstituted alkyl group having from 1 to about 10 carbon atoms; a cycloalkyl group having from about 5 to about 7 carbon atoms or an aryl group having from about 6 to about 10 carbon atoms; R 3 and R 4 each independently represents R 1 , with the proviso that at least one of R 3 and R 4 is hydrogen; R 5 represents hydrogen; halogen; cyano; a substituted or unsubstituted alkyl, alkylthio, alkylsulfonyl, alkylsulfinyl, alkoxycarbonyl, carbamoyl or alkoxy group having from 1 to about 10 carbon atoms; a substituted or unsubstituted arylthio, arylsulfonyl, arylsulfinyl, aryloxy or aryl group having from about 6 to about 10 carbon atoms; or a substituted or unsubstituted acylamido group having from about 1 to about 7 carbon atoms; and R 6 represents hydrogen; halogen; cyano; alkoxy; a substituted or unsubstituted alkyl group having from 1 to about 10 carbon atoms; a cycloalkyl group having from about 5 to about 7 carbon atoms or an aryl group having from about 6 to about 10 carbon atoms.
TL;DR: Several tricyclic benzopyrano[4,3-c]pyrazole derivatives have been studied by 1H and 13C n.m. spectroscopy as mentioned in this paper.
Abstract: Several tricyclic benzopyrano[4,3-c]pyrazole derivatives have been studied by 1H and 13C n.m.r. spectroscopy. They were prepared by treating 3-benzylidene-chromanones and -1-thiochromanones with semicarbazide or thiosemicarbazide: reactions which give only the cis 3-H,3a-H stereoisomers.
TL;DR: In this article, the structure of 2 has been determined by X-ray analysis and it is shown that the geometry about each copper atom is approximately a tetragonal bipyramid and the axial positions are occupied by two oxygen atoms one from each of the bidentate hfac ligands, the other oxygen atoms of which are in the basal plane with two nitrogen atoms from 4-Hmpz molecules.
Abstract: The preparation of Cu(hfac)2(4-Hmpz) (1), Cu(hfac)2(4-Hmpz)2 (2), and Cu(hfac)2(4-Hmpz)3 (3) by stoichiometric reactions of Cu(hfac)2 (Hhfac=1,1,1,5,5,5-hexafluoro-2,4-pentanedione) with 4-methyl-1H-pyrazole (4-Hmpz) in petroleum ether is reported. The structure of 2 has been determined by X-ray analysis. Crystal data for 2: triclinic, P\bar1, a=9.301(3), b=10.815(2), c=6.457(1) A, α=104.71(2), β=101.38(2), γ=75.41(2)°, V=601.8(3) A3, Z=1, and R=0.057. The geometry about each copper atom is approximately a tetragonal bipyramid. The axial positions are occupied by two oxygen atoms one from each of the bidentate hfac ligands, the other oxygen atoms of which are in the basal plane with two nitrogen atoms from 4-Hmpz molecules. The two nitrogen atoms are situated trans to each other. The axial oxygen atoms have a considerably long Cu–O(2) distance (2.346(3) A). In the IR spectrum of 2, unsplit ν C–O and ν N–H bands were observed at 1678 and 3441 cm−1, respectively. The structures of 1 and 3 are estimated on t...
TL;DR: The crystal structure of Sn(CHCH 2 ) 2 Cl 2 · 2C 3 H 4 N 2 has been determined in this paper, and the structure is centrosymmetric at the tin atom, with all trans-octahedral coordination geometry.
TL;DR: The thermal condensation at 200-300 o C of pyrazoles with substituted diethyl malonates or triethyl methanetricarboxylate yields the 1-oxo-1H-pyrazolo-[1,2-a] pyrazol-4-ium-3-olates as discussed by the authors.
Abstract: The thermal condensation at 200-300 o C of pyrazoles with substituted diethyl malonates or triethyl methanetricarboxylate yields the 1-oxo-1H-pyrazolo-[1,2-a] pyrazol-4-ium-3-olates
TL;DR: In this article, 3(5)-alkyl pyrazoles with ammonium nitrate and trifluoroacetic anhydride were obtained for double functionalisation of the pyrazole ring.
Abstract: Treatment of 3(5)-alkylpyrazoles with ammonium nitrate and trifluoroacetic anhydride in trifluoroacetic acid gives 3-alkyl-1,4-dinitropyrazoles directly. This procedure, in conjunction with cine-substitution, offers a direct route for double functionalisation of the pyrazole ring.3(5)-Cyano-5(3)-[(S)-2,3-diacetoxypropyl]-4-nitropyrazole (13), prepared in this way, was elaborated into 5-amino-3-[(S)-2,3-dihydroxypropyl]-1H-pyrazolo[4,3-d]pyrimidin-7(6H)-one (5), 7-amino-3-[(S)-2,3-dihydroxypropyl]-1H-6-methylpyrazolo[4,3-d]pyrimidin-5(6H)-one (6), its Ndemethyl analogue (7), and 4-amino-5-carbamoyl-3-[(S)-2,3-dihydroxypropyl]pyrazole (8), all of which are C-nucleoside analogues of the antiviral agent (S)-9-(2,3-dihydroxypropyl)adenine (4).
TL;DR: In this article, the product of the reduction of [Cu(pzH) 4 Cl 2 ] with Cu powder has been shown by single-crystal X-ray analysis to the dimeric species [Cu[PzH] 2 Cl] 2.