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4—氨基—2—氯吡啶的合成研究 总被引:4,自引:1,他引:3
在对4-氨基-2-氯吡啶合成路线进行分析评价的基础上,以2-氯吡啶-N-氧化物为起始原料,经过硝化和还原两步反应,者了以工业化为目的的合成研究,产品总收率达到56%。 相似文献
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2-巯基吡啶-1-氧化物(1)是广谱的抗菌剂,对革兰氏阳性菌、革兰氏阴性菌及真菌都有效。它可通过皮肤吸收,控制皮脂溢出性皮炎和头皮屑。文献报道,(1)的合成是以2-氯吡啶-1-氧化物为原料,经硫脲或硫化钠或硫氢化钠巯基化而制得。NO↓ClCNH2SH... 相似文献
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2—巯基吡啶的合成及结构测定 总被引:6,自引:0,他引:6
以2-氯吡啶为原料合成2-巯基吡啶(Ⅰ),产率60%。通过红外光谱、核磁共振和质谱对比化合物(Ⅰ)的结构进行了测试,证明合成方法的可靠性。. 相似文献
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The microwave‐assisted synthesis of two different types of N‐heterocyclic carbene‐palladium(II) complexes, (NHC)Pd(acac)Cl (NHC=N‐heterocyclic carbene; acac=acetylacetonate) and (NHC)PdCl2(3‐chloropyridine), has been carried out. A drastic reduction in reaction times (20 to 88 times faster, depending on the complex) was observed when compared to the previously described, conventionally‐heated synthesis of these complexes. The protocol also allowed for the synthesis of (IPr)Pd(acac)Cl [IPr=1,3‐bis(2,6‐diisopropylphenyl)imidazol‐2‐ylidene] on a 5‐mmol scale in 30 min, with the reactants loaded in air. 相似文献
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Carmen Barrera‐Ventura Dolors Salvatierra Francesc Giralt Jaume Giralt 《加拿大化工杂志》2013,91(6):1131-1139
Imidazole and 2‐chloropyridine were used as model molecules to investigate the acid hydrolysis kinetics of agrochemicals in high‐temperature water in a batch reactor system at 28 MPa. Pseudo‐first‐order hydrolysis reaction rate constants for the acid hydrolysis of Imidazole and 2‐chloropyridine were determined in the temperature ranges 200–600 and 400–575°C, respectively, at 28 MPa. Rate constants for both compounds increased with temperature with a local maximum observed at around 400°C due to changes in the physical properties of the solvent. Imidazole and 2‐chloropyridine conversions of 0.95 and 0.99999 were respectively attained at the highest temperature after 30 min of reaction. © 2012 Canadian Society for Chemical Engineering 相似文献
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农药中间体2—氯吡啶的光氯化合成研究 总被引:4,自引:0,他引:4
通过对吡啶光氯化的反应条件优化和化工控制,有效地控制了反应中的聚合, 焦油化等副反应,实现了反应的高转化率和高选择性.控制反应条件, 可以改变2-氯吡啶和2,6-二氯吡啶 两种产物的比例,使其中某一种产物为主.并用现代物理方法对主要产品之一的2-氯吡啶进行了结构分析,证实了这一合成方法的可靠性. 相似文献
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Naota Yokoyama Yuji Nakayama Hideki Nara Noboru Sayo 《Advanced Synthesis \u0026amp; Catalysis》2013,355(10):2083-2088
The well‐defined diphenylvinylphosphine‐palladium complex 1 and the diphenylcyclopropylphosphine‐palladium complex 2 were successfully synthesized. The crystal structures of these complexes were obtained by X‐ray crystallographic analysis. Both complexes were air‐ and moisture‐stable, and could be prepared on a gram scale. These palladium complexes catalyzed the Suzuki–Miyaura reaction of aryl bromides [turnover numbers (TON) up to 196,000] and aryl chlorides (TON up to 50,000). Furthermore, complex 2 catalyzed the Buchwald–Hartwig amination of aryl chlorides and aromatic/aliphatic amines with a low catalyst loading. These complexes showed different reactivities for the coupling of 2‐chloropyridine, and the origin of this difference is discussed. 相似文献
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Matthias G. J. Baud Patricia Haus Thomas Leiser Prof. Dr. Franz‐Josef Meyer‐Almes Dr. Matthew J. Fuchter 《ChemMedChem》2013,8(1):149-156
Novel picolinamide‐based histone deacetylase (HDAC) inhibitors were developed, drawing inspiration from the natural product psammaplin A. We found that the HDAC potency and isoform selectivity provided by the oxime unit of psammaplin A could be reproduced by using carefully chosen heterocyclic frameworks. The resulting (hetero)aromatic amide based compounds displayed very high potency and isoform selectivity among the HDAC family, in addition to excellent ligand efficiency relative to previously reported HDAC inhibitors. In particular, the high HDAC1 isoform selectivity provided by the chloropyridine motif represents a valuable design criterion for the development of new lead compounds and chemical probes that target HDAC1. 相似文献
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Chao Wang Zhaoqing Xu Tomas Tobrman Ei‐ichi Negishi 《Advanced Synthesis \u0026amp; Catalysis》2010,352(4):627-631
The hitherto unprecedented palladium‐catalyzed cross‐coupling of (Z)‐β‐bromo‐β‐arylethenylboranes can be made to proceed satisfactorily through (1) the use of highly catalytically active bis(tri‐tert‐butylphosphine)palladium or dichloro[N,N‐bis‐(2,6‐diisopropylphenyl)imidazol‐2‐yl](m‐chloropyridine)palladium and (2) conversion of the dibromoboryl group to the (pinacol)boryl group. Thus, a wide variety of carbon groups can be used to substitute bromine in ≥98% stereo‐ and regioselectivity, while suppressing the otherwise dominant β‐debromoboration. Together with the alkylethyne‐based protocols, the alkyne bromoboration–Negishi coupling tandem process has emerged as the most widely applicable and highly selective route to trisubstituted alkenes including those that are otherwise difficult to access. 相似文献
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Brands M Ergüden JK Hashimoto K Heimbach D Krahn T Schröder C Siegel S Stasch JP Tsujishita H Weigand S Yoshida NH 《ChemMedChem》2006,1(1):96-105
Inhibition of the metalloprotease ECE-1 may be beneficial for the treatment of coronary heart disease, cancer, renal failure, and urological disorders. A novel class of indole-based ECE inhibitors was identified by high throughput screening. Optimization of the original screening lead structure 6 led to highly potent inhibitors such as 11, which bears a bisaryl amide moiety linked to the indole C2 position through an amide group. Docking of 11 into a model structure of ECE revealed a unique binding mode in which the Zn center of the enzyme is not directly addressed by the inhibitor, but key interactions are suggested for the central amide group. Testing of the lead compound 6 in hypertensive Dahl S rats resulted in a decrease in blood pressure after an initial period in which the blood pressure remained unchanged, most probably the result of ET-1 already present. Indole derivative 6 also displays a cardio-protective effect in a mouse model of acute myocardial infarction after oral administration. The more potent chloropyridine derivative 9 antagonizes big-ET-1-induced increase in blood pressure in rats at intravenous administration of 3 mg kg-1. All ECE inhibitors of the indole class showed high selectivity for ECE over related metalloproteases such as NEP and ACE. Therefore, these compounds might have further potential as drugs for the treatment of coronary heart diseases. 相似文献
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Dr. Christopher L. Schardon Dr. Alfred Tuley Dr. Joyce A. V. Er Jake C. Swartzel Dr. Walter Fast 《Chembiochem : a European journal of chemical biology》2017,18(15):1551-1556
We have investigated 4‐halopyridines as selective, tunable, and switchable covalent protein modifiers for use in the development of chemical probes. Nonenzymatic reactivity of 4‐chloropyridine with amino acids and thiols was ranked with respect to common covalent protein‐modifying reagents and found to have reactivity similar to that of acrylamide, but could be switched to a reactivity similar to that of iodoacetamide upon stabilization of the positively charged pyridinium. Diverse, fragment‐sized 4‐halopyridines inactivated human dimethylarginine dimethylaminohydrolase‐1 (DDAH1) through covalent modification of the active site cysteine, acting as quiescent affinity labels that required off‐pathway catalysis through stabilization of the protonated pyridinium by a neighboring aspartate residue. A series of 2‐fluoromethyl‐substituted 4‐chloropyridines demonstrated that the pKa and kinact/KI values could be predictably varied over several orders of magnitude. Covalent labeling of proteins in an Escherichia coli lysate was shown to require folded proteins, indicating that alternative proteins can be targeted, and modification is likely to be catalysisdependent. 4‐Halopyridines, and quiescent affinity labels in general, represent an attractive strategy to develop reagents with switchable electrophilicity as selective covalent protein modifiers. 相似文献