3-(3-吲哚基)-5-吡唑甲酰胺的合成及抑菌活性

本文以3-乙酰吲哚、草酸二乙酯、水合肼等为原料,经缩合、环化、水解反应制备3-(3-吲哚基)吡唑-5-甲酸,后者再与苄胺或2-苯乙胺在EDC-BTOH催化下合成了一系列N-取代苄基-3-(3-吲哚基)吡唑-5-甲酰胺和N-(2-取代苯基乙基)-3-(3-吲哚基)吡唑-5-甲酰胺。采用平板计数法测试了化合物对大肠杆菌和金黄色葡萄球菌的抑制活性,结果表明,在浓度为80 μg/mL时部分化合物有较高的抑菌活性。     

ChemInform Abstract: Study of the Linkage Isomerization (Co(NH3)5NO2)Br2 ⇌ (Co(NH3) 5ONO)Br2 in the Solid State by X-Ray Powder Diffraction.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

ChemInform Abstract: Crystallographic Data for New Ternary UCo5Si3-Type LnRh5Si3 (Ln: Sm,Gd—Tm) Compounds.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

ChemInform Abstract: Crystal Structures of La3ZrSb5, La3HfSb5, and LaCrSb3. Structural Relationships in Ternary Rare-Earth Antimonides.

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 100 leading journals. To access a ChemInform Abstract of an article which was published elsewhere, please select a “Full Text” option. The original article is trackable via the “References” option.     

Sr3Cu5O8＋x和CaSrCu5O5＋x的结构和电学性质

继Y-Ba-Cu-O之后,具有更高T_5的Bi-Sr-Ca-Cu-O(简称BSCCO)体系的发现引起了人们对高温超导研究的兴趣。研究表明,在BSCCO中存在110K和80K2个超导相。由于在制备BSCCO过程中存在复杂的Ca、Sr和Cu复合氧化物,要得到稳定的110K相相当困     

Neue Untersuchungen zum Reaktionsverhalten von Triorganylcyclotriphosphanen. Die Kristallstrukturen von [(PPh3)2Pt(PtBu)3], [(PPh3)2Pd(PtBu)2], [(CO)4Cr{(PiPr)3}2], [RhCl(PPh3)(PtBu)3], [(NiCO)6(μ2-CO)3{(PtBu)2}2] und [(CpFeCO)2(μ-CO)(μ-PHtBu)]+ · [FeCl3(thf)]–

New Research of Reaction Behaviour of Triorganylcyclotriphosphines. The Crystal Structures of [(PPh₃)₂Pt(P^tBu)₃], [(PPh₃)₂Pd(P^tBu)₂], [(CO)₄Cr{(PⁱPr)₃}₂], [RhCl(PPh₃)(P^tBu)₃], [(NiCO)₆(μ₂-CO)₃{(P^tBu)₂}₂], and [(CpFeCO)₂(μ-CO)(μ-PH^tBu)]⁺ · [FeCl₃(thf)]^– By the reaction of triorganylcyclotriphosphines with transition metal complexes single- and polynuclear compounds are formed, in which the cyclophosphines are bonded in different ways to the metal, the ring either preserving structure or under going ring opening. Depending on the reaction conditions the following compounds can be characterized: [(PPh₃)₂Pt(P^tBu)₃] ( 1 ), [(PPh₃)₂Pd(P^tBu)₂] ( 2 ), [(CO)₄Cr{(PⁱPr)₃}₂] ( 3 ), [RhCl(PPh₃)(P^tBu)₃] ( 4 ), [(NiCO)₆(μ₂-CO)₃{(P^tBu)₂}₂] ( 5 ) and [(CpFeCO)₂(μ-CO)(μ-PH^tBu)]⁺ · [FeCl₃(thf)]^– ( 6 ). The structures of 1 – 6 were obtained by X-ray single crystal structure analysis ( 1 : space group P2₁/n (No. 14), Z = 4, a = 1279.6(3) pm, b = 1733.1(4) pm, c = 2079.1(4) pm, β = 90.20(3)°; 2 : space group P2₁/c (No. 14), Z = 4, a = 1053.3(2) pm, b = 2085.2(4) pm, c = 1855.7(4) pm, β = 98.77(3)°; 3 : space group P 1 (No. 2), Z = 2, a = 1022.6(2) pm, b = 1026.4(2) pm, c = 1706.0(3) pm, α = 82.36(3)°, β = 86.10(3)°, γ = 64.40(3)°; 4 : space group P 1 (No. 2), Z = 2, a = 980.2(2) pm, b = 1309.5(3) pm, c = 1573.4(3) pm, α = 99.09(3)°, β = 99.46(3)°, γ= 111.87(3)°; 5 : space group P2₁/c (No. 14), Z = 4, a = 1804.0(5) pm, b = 2261.2(6) pm, c = 1830.1(7) pm, β = 96.99(3)°; 6 : space group P2₁/c (No. 14), Z = 4, a = 943.2(3) pm, b = 2510.6(7) pm, c = 1325.1(6) pm, β = 98.21(3)°).     

Synthesis and structure of 1-(4-chlorophenyl)-3-(5-methyl-1, 3-dioxan-5-yl)-(1,2),(3,4)-diepoxybutane

The synthesis and X-ray structural study of 1-(4-chlorophenyl)-3-(5-methyl-1,3-dioxan-5-yl)-(1,2), (3,4)-diepoxybutane are described.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 4, pp. 715–718, April, 1995.     

Synthesen und Eigenschaften von Tetrakis(perfluoralkyl)tellur Te(Rf)4 (Rf = CF3, C2F5, C2F5, C3F7, C4F9)

Synthesis and Properties of Tetrakis(Perfluoroalkyl)Tellurium Te(R_f)₄ (R_f = CF₃, C₂F₅, C₃F₇, C₄F₉) Te(CF₃)₄ is obtained from the reaction of Te(CF₃)Cl₂ with Cd(CF₃)₂ complexes as a complex with e. g. CH₃CN, DMF. It is a light and temperature sensitive hydrolysable liquid. The reaction with fluorides yields the complex anion [Te(CF₃)₄F]⁻, with fluoride ion acceptors the complex cation [Te(CF₃)₃]⁺. With traces of water an acidic solution is formed. Te(CF₃)₄ acts as a trifluoromethylation reagent. The reaction with XeF₂ gives hints for the formation of Ye(CF₃)₄F₂. Properties and NMR spectra are discussed. The much more stable complexes of Te(R_f)₄ (R_f = C₂F₅, C₃F₇, C₄F₉) are formed from the reaction of TeCl₄ with the corresponding Cd(R_f)₂ complexes.     

NEW AND CONVENIENT SYNTHESIS OF (R) AND (S) OF 2-METHYL-3-OXA-5-(TERT-BUTYLDIPHENYLSILYLOXYL) METHYLPENTANOATE AND 2-METHYL-3-OXA-5- (TERT-BUTYLDIMETHYLSILYLOXYL)METHYLPENTANOATE

Abstract

(R) and (S) of 2-Methy1-3-oxa-5-(tert-butyldiphenylsilyloxyl)methy1pentanoate (4a. 6a) and (R) and (S) of 2-methy1-3-oxa-5-(tert-butyldimethylsilyloxyl)methylpentanoate (4b, 6b) were synthesized by the reaction of the preparative compounds (2a, 2b) with (R) and (S) methy1lactate (3, 4) in the presence of a silver (1) oxide catalyst (Method B). The title compounds are useful for the synthesis of different natural products such as epothilones.     

Synthesis and Characterization of Novel Methyl (3)5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates

Series of methyl 3- and 5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates were developed and regioselectively synthesized as novel heterocyclic amino acids in their N-Boc protected ester form for achiral and chiral building blocks. In the first stage of the synthesis, piperidine-4-carboxylic and (R)- and (S)-piperidine-3-carboxylic acids were converted to the corresponding β-keto esters, which were then treated with N,N-dimethylformamide dimethyl acetal. The subsequent reaction of β-enamine diketones with various N-mono-substituted hydrazines afforded the target 5-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates as major products, and tautomeric NH-pyrazoles prepared from hydrazine hydrate were further N-alkylated with alkyl halides to give 3-(N-Boc-piperidinyl)-1H-pyrazole-4-carboxylates. The structures of the novel heterocyclic compounds were confirmed by ¹H-, ¹³C-, and ¹⁵N-NMR spectroscopy and HRMS investigation.     

ORGANIC PHOSPHORUS COMPOUNDS 93.1 PREPARATION,PROPERTIES AND HERBICIDAL ACTIVITY OF 2-SUBSTITUTED 5-PHENOXY- AND 5-PYRIDY LOXY-PHENYLAMINOALKYLPHOSPHONIC-AND-PHOSPHINIC ACILAS WELL AS-PHOSPHINE OXIDE DERIVATIVES*

Abstract

Interaction of 4-phenoxy and 4-pyridyloxy substituted 1.2-dinitrobenzenes and aminoalkylphosphonates,-phosphinates, and -phosphine oxides produces mainly 5-phenoxy- and 5-pyridyloxy substituted 2-nitrophenylaminoalkyIphosphonates. -phosphinates and -phosphine oxides (Table I to IV and Figure 1 to 5). some of which show high herbicidal and plant growth regulating activity. The herbicidal activity increases from pyridyloxy-phenylaminoalkylphosphonates to phenoxy-phenylaminoalkyl-phosphonates, -phosphinates, -phosphine oxides. Of all the compounds tested the phosphine oxide 4a was at all concentrations the most active compound.