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51.
Brendan Frett Nicholas McConnell Anupreet Kharbanda Gunaganti Naresh Benjamin Rounseville Christina Warner John Chang Natalie Debolske Hong-yu Li 《Tetrahedron》2018,74(35):4592-4600
Carbon-carbon bonds are integral for pharmaceutical discovery and development. Frequently, CC bond reactions utilize expensive catalyst/ligand combinations and/or are low yielding, which can increase time and expenditures in pharmaceutical development. To enhance CC bond formation protocols, we developed a highly efficient, selective, and combinatorially applicable Friedel-Crafts acylation to acetylate the C-3 position of imidazo[1,2-a]pyridines. The reaction, catalyzed by aluminum chloride, is both cost effective and more combinatorial friendly compared to acetylation reactions requiring multiple, stoichiometric equivalents of AlCl3. The protocol has broad application in the construction of acetylated imidazo[1,2-a]pyridines with an extensive substrate scope. All starting materials are common and the reaction requires inexpensive, conventional heating methods for adaptation in any laboratory. Further, the synthesized compounds are predicted to possess GABA activity through a validated, GABA binding model. The developed method serves as a superior route to generate C-3 acetylated imidazo[1,2-a]pyridine building-blocks for combinatorial synthetic efforts. 相似文献
52.
Rouhana Nathalie Handagama Naresh Bienkowski Paul R. 《Applied biochemistry and biotechnology》1997,(1):809-821
A vapor-phase bioreactor has been developed utilizing porous metal membranes in a cylindrical design employing radial flow
as opposed to traditional axial flow for the vapor stream. The system was evaluated for the biodegradation ofp-xylene (p-xylene) from a water-saturated air stream byPseudomonas putida ATCC 23973 immobilized onto sand. The biocatalyst was placed in the annular space between two cylindrical, porous stainless-steel
membranes. Details of the reactor system are presented along with biological data verifying system performance. The feed flow
rate andp-xylene concentration were varied between 60 and 130 cm3/min and 15–150 ppm, respectively. Continuous reactor operation was maintained for 80–200 h with removal efficiencies (based
onp-xylene disappearance) between 80 and 95%. The effluent concentration histories were compared to determine the operating range
of the bioreactor. 相似文献
53.
Spectroscopic investigation of a dihydrogen-bonded complex between phenol and triethylgermanium hydride is reported here. Laser-induced fluorescence excitation, fluorescence-detected infrared, and IR-UV hole-burning spectroscopic studies were carried out in supersonic jet to investigate the complex formation between phenol and triethylgermanium hydride. The lowering of the O-H stretching frequency of the phenol moiety in the complex with triethylgermanium hydride clearly establishes the role of phenol as hydrogen bond donor. The experimental results together with the ab-initio calculations unambiguously confirm formation of an O-H...H-Ge dihydrogen-bonded complex between phenol and triethylgermanium hydride. 相似文献
54.
The electronic transitions of phenylacetylene complexes with water and trifluoroethanol are shifted to the blue, while the corresponding transitions for methanol and ethanol complexes are shifted to the red relative to the phenylacetylene monomer. Fluorescence dip infrared (FDIR) spectra in the O-H stretching region indicate that, in all the cases, phenylacetylene is acting as a hydrogen bond acceptor to the alcohols. The FDIR spectrum in the acetylenic C-H stretching region shows Fermi resonance bands for the bare phenylacetylene, which act as a sensitive tool to probe the intermolecular structures. The FDIR spectra reveal that water and trifluoroethanol interact with the pi electron density of the acetylene C-C triple bond, while methanol and ethanol interact with the pi electron density of the benzene ring. It can be inferred that the hydrogen bonding acceptor site on phenylacetylene switches from the acetylene pi to the benzene pi with lowering in the partial charge on the hydrogen atom of the OH group. The most significant finding is that the intermolecular structures of water and methanol complexes are notably distinct, which, to the best of our knowledge, this is first such observation in the case of complexes of substituted benzenes. 相似文献
55.
Valeriu Mereacre Denis Prodius Ayuk M. Ako Narpinder Kaur Janusz Lipkowski Charles Simmons Naresh Dalal Ion Geru Christopher E. Anson Annie K. Powell Constantin Turta 《Polyhedron》2008
Reaction of manganese acetate and lanthanide nitrates in the presence of excess of PhCOOH affords highly asymmetric dodecanuclear mixed-metal [Mn10Ln2(OH)(O)8(PhCOOH)(PhCOO)19] (Ln = PrIII (1), NdIII (2)) clusters. The similar reaction, but with only 2 equiv. of PhCOOH resulted in the compounds with higher nuclearity [Mn11Eu4(O)8(OH)8(PhCOO)18(NO3)2(H2O)6]NO3 · 4CH3CN (3). Variable-temperature solid-state magnetic susceptibility of 1 and 2 in the temperature range 1.8–300 K were carried out, and for both complexes antiferromagnetic exchange interactions between the metal centers were observed, giving an estimated S = 17/2 ground state. AC magnetic susceptibility data have revealed out-of-phase signals, which suggest that these complexes exhibit a slow relaxation of magnetization as observed in single-molecule magnets. 相似文献
56.
Parvateesam Yenda Naresh Kumar Katari Balasubramanian Satheesh Rambabu Gundla Siva Krishna Muchakayala Vijay Kumar Rekulapally 《Journal of separation science》2023,46(11):2200770
The design of an appropriate analytical method for assessing the quality of pharmaceuticals requires a deep understanding of science, and risk evaluation approaches are appreciated. The current study discusses how a related substance method was developed for Nintedanib esylate. The best possible separation between the critical peak pairs was achieved using an X-Select charged surface hybrid Phenyl Hexyl (150 × 4.6) mm, 3.5 μm column. A mixture of water, acetonitrile, and methanol in mobile phase-A (70:20:10) and mobile phase-B (20:70:10), with 0.1% trifluoroacetic acid and 0.05% formic acid in both eluents. The set flow rate, wavelength, and injection volumes were 1.0 ml/min, 285 nm, and 5 μl, respectively, with gradient elution. The method conditions were validated as per regulatory requirements and United States Pharmacopeia general chapter < 1225 >. The correlation coefficient for all impurities from the linearity experiment was found to be > 0.999. The % relative standard deviation from the precision experiments ranged from 0.4 to 3.6. The mean %recovery from the accuracy study ranged from 92.5 to 106.5. Demonstrated the power of the stability-indicating method through degradation studies; the active drug component is more vulnerable to oxidation than other conditions. Final method conditions were further evaluated using a full-factorial design. The robust method conditions were identified using the graphical optimization from the design space. 相似文献
57.
Chevella Durgaiah Mameda Naresh Macharla Arun Kumar Peraka Swamy Marri Mahender Reddy Kodumuri Srujana 《合成通讯》2016,46(13):1133-1144
A simple, efficient, and environmentally benign protocol for the synthesis of vicinal iodohydrins and iodoesters from olefins using NH4I and Oxone in CH3CN/H2O (1:1) and dimethylformamide (DMF) / dimethylacetamide (DMA), respectively, without employing a catalyst at room temperature is described. Regio- and stereoselective iodohydroxylation and iodoesterification of various olefins with anti fashion, following Markonikov’s rule, was achieved and the corresponding products were obtained in good to excellent yields. In addition, 1,2-disubstituted olefins afforded excellent diastereoselectivity. 相似文献
58.
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60.
Vivek K. Gupta Madhvi M. Lal Naresh K. Satti Prabhu Dutt Punita Sharma Musarat Amina Krishan A. Suri 《Journal of chemical crystallography》2011,41(7):1064-1070