- Charge-directed conjugate addition reactions of salts of unsaturated β-keto-esters
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Strong nucleophiles undergo conjugate addition reactions with enolates of Nazarov-type reagents. Yields are strongly affected by substitution patterns and the metal cation employed.
- Cooke Jr.,Jaw
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Read Online
- Discrimination of β-ketoesters by ruthenium(II)-binap-catalyzed asymmetric hydrogenation
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(Chemical Equation Presented) Please, after you... β-Ketoesters in mixtures underwent Noyori reduction one by one at room temperature under 4 bar of hydrogen pressure in the presence of a catalyst formed from RuII and (S)-binap (see example). The rate of the asymmetric hydrogenation and hence the selectivity for a particular β-ketoester was found to depend on the Lewis basicity of the ester group. Binap = 2,2′-bis(diphenylphosphanyl)-1, 1′-binaphthyl.
- Kramer, Rainer,Brueckner, Reinhard
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Read Online
- Radical Aza-Cyclization of α-Imino-oxy Acids for Synthesis of Alkene-Containing N-Heterocycles via Dual Cobaloxime and Photoredox Catalysis
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Nitrogen-containing heterocycles are prevalent in both naturally and synthetically bioactive molecules. We report herein an unprecedented protocol for radical aza-cyclization of α-imino-oxy acids with pendant alkenes via synergistic photoredox and cobaloxime catalysis. With or without alkenes as the intermolecular cross-coupling partners, the transformation provides a variety of corresponding alkene-containing dihydropyrrole products in satisfactory yields. In the presence of external alkenes, the tandem reaction generates E-selective coupling products with excellent chemo- and stereoselectivity.
- Tu, Jia-Lin,Liu, Jia-Li,Tang, Wan,Su, Ma,Liu, Feng
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supporting information
p. 1222 - 1226
(2020/02/15)
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- Desymmetrization of meso-dicarbonatecyclohexene with β-Hydrazino carboxylic esters via a Pd-catalyzed allylic substitution cascade
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The desymmetrization of meso-dicarbonatecyclohexene with β-hydrazino carboxylic esters has been achieved via a RuPHOX/Pd-catalyzed allylic substitution cascade for the construction of chiral hexahydrocinnoline derivatives with high performance. Mechanistic studies reveal that the reaction exploits a pathway different from that of our previous work and that the first nitrogen nucleophilic process is the rate-determining step. The protocol could be conducted on a gram scale without any loss of catalytic behavior, and the corresponding chiral hexahydrocinnolines can undergo diverse transformations.
- Xu, Kai,Zheng, Yan,Ye, Yong,Liu, Delong,Zhang, Wanbin
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supporting information
p. 8836 - 8841
(2020/11/30)
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- Synthesis of Long-Chain β-Lactones and Their Antibacterial Activities against Pathogenic Mycobacteria
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In the quest for new antibacterial agents, a series of novel long- and medium-chain mono- and disubstituted β-lactones was developed. Their activity against three pathogenic mycobacteria—M. abscessus, M. marinum, and M. tuberculosis—was assessed by the resazurin microtiter assay (REMA). Among the 16 β-lactones synthesized, only 3-hexadecyloxetan-2-one (VM005) exhibited promising activity against M. abscessus, whereas most of the β-lactones showed interesting activities against M. marinum, similar to that of the classical antibiotic, isoniazid. Regarding M. tuberculosis, six compounds were found to be active against this mycobacterium, with β-lactone VM008 [trans-(Z)-3-(hexadec-7-en-1-yl)-4-propyloxetan-2-one] being the best growth inhibitor. The promising antibacterial activities of the best compounds in this series suggest that these molecules may serve as leads for the development of much more efficient antimycobacterial agents.
- Santucci, Pierre,Dedaki, Christina,Athanasoulis, Alexandros,Gallorini, Laura,Munoz, Ana?s,Canaan, Stéphane,Cavalier, Jean-Fran?ois,Magrioti, Victoria
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supporting information
p. 349 - 358
(2019/01/25)
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- General [4 + 1] Cyclization Approach to Access 2,2-Disubstituted Tetrahydrofurans Enabled by Electrophilic Bifunctional Peroxides
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A general [4 + 1] cyclization reaction of carbonyl nucleophiles with 2-iodomethylallyl peroxides, which function as unique electrophilic oxygen synthons, for the synthesis of a broad range of 2,2-disubstituted tetrahydrofurans is achieved under operationally simple conditions. The unprecedented asymmetric version of such reaction is also realized via chiral auxiliary-assisted cyclization, thus providing a distinct approach to access chiral tetrahydrofurans with high diastereoselectivities. The new method can be applied to the synthesis of core structure of posaconazole drug.
- Gao, Min,Zhao, Yukun,Zhong, Chen,Liu, Shengshu,Liu, Pengkang,Yin, Qi,Hu, Lin
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supporting information
p. 5679 - 5684
(2019/08/01)
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- Continuous flow synthesis of toxic ethyl diazoacetate for utilization in an integrated microfluidic system
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An integrated microfluidic system for multiple reactions and separations of hazardous ethyl diazoacetate is presented. The integrated techniques include: a droplet technique for liquid-liquid and/or gas-liquid separation and in situ generation of the toxic reagent, a dual channel membrane technique based on a cheap polymeric microseparator for liquid-liquid separation, and a capillary microreactor for carrying out cascade reactions in a sequential and continuous manner.
- Maurya, Ram Awatar,Min, Kyoung-Ik,Kim, Dong-Pyo
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supporting information
p. 116 - 120
(2014/01/06)
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- Tert-BuOK-Catalyzed condensation of ethyl diazoacetate to aldehydes and palladium-catalyzed 1,2-hydrogen migration for the synthesis of β-ketoesters under solvent-free conditions
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A mild and convenient method for the condensation of ethyl diazoacetate (EDA) with aldehydes catalyzed by tert-BuOK under solvent-free conditions was developed. The corresponding α-diazo-β-hydroxy esters were further converted into β-ketoesters through palladium-catalyzed 1,2-hydrogen migration under neat conditions. The two-step transformation exemplifies a simple method for the efficient and green synthesis of β-ketoesters. The Royal Society of Chemistry 2013.
- Chen, Shufeng,Yuan, Fang,Zhao, Haiying,Li, Baoguo
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p. 12616 - 12620
(2013/08/23)
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- Chemoenzymatic asymmetric synthesis of pregabalin precursors via asymmetric bioreduction of β-cyanoacrylate esters using ene-reductases
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The asymmetric bioreduction of a library of β-cyanoacrylate esters using ene-reductases was studied with the aim to provide a biocatalytic route to precursors for GABA analogues, such as pregabalin. The stereochemical outcome could be controlled by substrate-engineering through size-variation of the ester moiety and by employing stereochemically pure (E)- or (Z)-isomers, which allowed to access both enantiomers of each product in up to quantitative conversion in enantiomerically pure form. In addition, stereoselectivities and conversions could be improved by mutant variants of OPR1, and the utility of the system was demonstrated by preparative-scale applications.
- Winkler, Christoph K.,Clay, Dorina,Davies, Simon,O'Neill, Pat,McDaid, Paul,Debarge, Sebastien,Steflik, Jeremy,Karmilowicz, Mike,Wong, John W.,Faber, Kurt
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p. 1525 - 1533
(2013/04/10)
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- PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS
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The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Mvraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotynebacterium, Bacillus spp., Enterobactericeae (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections.
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Paragraph 0432; 0433
(2015/04/15)
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- Sodium borohydride/methoxydiethylborane mediated syn-1,3-stereoselective total synthesis of herbarumin-III
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A simple and efficient stereoselective total synthesis of 10-membered macrolide, herbarumin-III is described. The key steps involved in this synthesis are the selective terminal alkylation of ethyl acetoacetate with ethyl bromide, Sharpless epoxidation, NaBH4/Et2BOMe mediated stereoselective syn-1,3-asymmetric reduction, esterification and olefin metathesis.
- Yadav,Narasimhulu,Vikram Reddy,Subba Reddy,Al Khazim Al Ghamdi, Ahmad
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experimental part
p. 1075 - 1082
(2011/10/02)
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- Synthesis of Biginelli dihydropyrimidinone derivatives with various substituents on aluminium-planted mesoporous silica catalyst
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Biginelli reactions were well catalyzed on mesoporous silica MCM-41 (M41) whose activity was much greater than that of amorphous silica. Octane was the most suitable among 6 kinds of solvents examined. The addition of metal ions on M41 enhanced the catalytic activity in the order Al > Ti > Fe = In. Al-planted M41s with Si/Al ratios of 45-35 showed the highest catalytic activity and could be used repeatedly though a small loss of the activity was observed. The catalysis could widely be applied to obtain various substituted dihydropyrimidinones (DHPMs) with high yields, some of which were very difficult to prepare until now. In addition, Biginelli reactions were combined with formyl C-H insertion reactions of diazoester on mesoporous silica; that is, a tandem one-pot four-component DHPM synthesis was attempted. Acetaldehyde, ethyl diazoacetate, p-tolualdehyde, and urea could be condensed and the corresponding DHPM derivative was obtained with 50% yield on Al-planted M41. The Royal Society of Chemistry.
- Murata, Hiroaki,Ishitani, Haruro,Iwamoto, Masakazu
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experimental part
p. 1202 - 1211
(2010/06/13)
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- PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS
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The present invention provides DNA Gyrase and/or Topo IV inhibitors of formula I, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonus spp., Acenetobacter spp., Muraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Mycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Cotyne bacterium, Bacillus spp., Enterobactericeae (E.coli, Klebsiella spp., Proteus spp.,etc.) or any combination thereof Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections
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Page/Page column 65
(2010/04/03)
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- AMIDE COMPOUND AND BACTERIAL DISEASE CONTROL AGENT FOR AGRICULTURAL AND HORTICULTURAL USE
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The present invention provides an amide compound having antibacterial activity, and a bacterial infection control agent for agricultural and horticultural use that contains the amide compound. The novel amide compound of the present invention is represented by General Formula (1): wherein R is a -CH(R1)(R2) or a -CO(R2) group, R1 is a hydrogen atom or a hydroxyl group, and R2 is a C1-12 alkyl group.
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Page/Page column 7-8
(2010/09/05)
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- A double Mannich approach to the synthesis of substituted piperidones - Application to the synthesis of substituted E-ring analogues of methyllycaconitine
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The double Mannich reaction of acyclic α,γ-substituted β-keto esters and bis(aminol) ethers gives substituted 3,5-substituted-4- piperidones with high levels of diastereoselectivity. These piperdiones can be easily transformed into substituted E-ring analogues of the delphinium alkaloid methyllycacotine.
- Chan, Yinman,Balle, Jared,Kevin Sparrow,Boyd, Peter D.W.,Brimble, Margaret A.,Barker, David
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experimental part
p. 7179 - 7191
(2010/10/01)
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- AMIDE COMPOUND, SALT THEREOF, AND BIOFILM REMOVER USING THEM
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The present invention provides a biofilm stripping agent for removing biofilms already formed. The biofilm stripping agent of the present invention contains, as an active ingredient, an amide compound or salt thereof denoted by General Formula (1), wherein R is a C1-11 alkyl group, and Q is a substituent denoted by the following Formulas (Q1), (Q2) or (Q3), wherein, in Formula (Q1), n is an integer ranging from 0 to 4; in Formula (Q2), R1 is a C1-4 alkyl group, and R2 is a hydroxyl group or carbamoyl group; in Formula (Q3), R3 is a hydrogen atom, hydroxyl group or carbamoyl group.
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Page/Page column 13-14
(2009/07/18)
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- Selective synthesis of α-substituted β-keto esters from aldehydes and diazoesters on mesoporous silica catalysts
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The titled reactions are effectively catalyzed on mesoporous silica MCM-41 but not on amorphous silica prepared from the same starting materials as those of MCM-41. The ordered porous structure was essential to generate the acid catalysis. Planting of Al or Ti ion improved not only the catalytic activity but also the tolerance to basic functional groups of substrates. The catalytic activity of Al- or Ti-MCM-41 was better than that of SnCl2 and NbCl5 in the homogeneous phase. In particular, Al (or Ti)-MCM-41 was characteristically active for the reaction of aldehydes with α-substituted diazoesters to give 2-substituted-3-oxo propionic acid esters.
- Murata, Hiroaki,Ishitani, Haruro,Iwamoto, Masakazu
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p. 4788 - 4791
(2008/12/22)
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- Substitution of acyl for acetyl with N-acylbenzotriazoles catalyzed by samarium triiodide
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Catalyzed by samarium triiodide (SmI3), substitution of acyl with N-acylbenzotriazoles for acetyl in acetoacetic esters and acetylacetone proceeds smoothly under neutral conditions in open air, affording the corresponding β-keto esters and β-diketones in good yields. Copyright Taylor & Francis Group, LLC.
- Zou, Xuefei,Jia, Xiaofei,Wang, Xiaoxia,Xie, Guanqun
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p. 1617 - 1625
(2008/02/01)
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- Nitroalkanes and ethyl glyoxalate as common precursors for the preparation of both β-keto esters and α,β-unsaturated esters
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β-Nitro acrylic esters, obtained by the reaction of nitroalkanes and ethyl glyoxalate, are the key building blocks for the immediate synthesis of both the title compounds. In fact, their treatment with titanium trichloride produce the direct conversion to the β-keto esters, while their reaction with sodium boron hydride gives the one-pot synthesis of α,β- unsaturated esters through formal substitution of the vinylic nitro group with an hydrogen.
- Ballini, Roberto,Fiorini, Dennis,Palmieri, Alessandro
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p. 7027 - 7029
(2007/10/03)
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- Novel isoxazole carboxamides as growth hormone secretagogue receptor (GHS-R) antagonists
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Novel isoxazole carboxamides have been identified as growth hormone secretagogue receptor (GHS-R) antagonists. Substituent modification off the 5-position of the isoxazole ring led to analogues with potent binding affinity and functional antagonism of GHS-R. A potent analogue (32) with high aqueous solubility and good GPCR selectivity was also identified as a potential pharmacological tool for in vivo studies.
- Liu, Bo,Liu, Gang,Xin, Zhili,Serby, Micheal D.,Zhao, Hongyu,Schaefer, Verlyn G.,Falls, H. Douglas,Kaszubska, Wiweka,Collins, Christine A.,Sham, Hing L.
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p. 5223 - 5226
(2007/10/03)
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- Efficient activation of zinc: Application of the Blaise reaction to an expedient synthesis of a statin intermediate
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Efficient and practical in situ zinc activation was accomplished by treatment with catalytic amount of an organic acid. The protocol was applied successfully to the Blaise reaction of various nitriles. Noteworthy is the excellent Blaise transformation of (S)-4-chloro-3-trimethylsilyloxybutyronitrile (2b) into tert-butyl (S)-6-chloro-5-hydroxy-3-oxohexanoate (1), a key intermediate for the preparation of HMG-CoA reductase inhibitors (statins).
- Shin, Hyunik,Choi, Bo Seung,Lee, Ki Kon,Choi, Hyeong-Wook,Chang, Jay Hyok,Lee, Kyu Woong,Nam, Do Hyun,Kim, No-Soo
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p. 2629 - 2632
(2007/10/03)
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- A general synthesis of dioxolenone prodrug moieties
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A general method for the synthesis of dioxolenone prodrug moieties from appropriately substituted β-ketoesters is described. This novel and versatile sequence allows for the synthesis of alkyl- or aryl-substituted dioxolenone alcohols 8 or bromides 9. Coupling of the bromides 9 to prepare bis-dioxolenone phosphonate prodrug esters is also presented.
- Sun, Chong-Qing,Cheng, Peter T.W.,Stevenson, Jay,Dejneka, Tamara,Brown, Baerbel,Wang, Tammy C.,Robl, Jeffrey A.,Poss, Michael A.
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p. 1161 - 1164
(2007/10/03)
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- Discovery of a series of pyrrolidine-based endothelin receptor antagonists with enhanced ET(A) receptor selectivity
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Endothelins, ET-1, ET-2, and ET-3 are potent vasoconstricting and mitogenic 21-amino acid bicyclic peptides, which exert their effects upon binding to the ET(A) and ET(B) receptors. The ET(A) receptor mediates vasoconstriction and smooth muscle cell proliferation, and the ET(B) receptor mediates different effects in different tissues, including nitric oxide release from endothelial cells, and vasoconstriction in certain vascular cell types. Selective antagonists of endothelin receptor subtypes may prove useful in determining the role of endothelin in various tissue types and disease states, and hence as therapeutic agents for such diseases. The pyrrolidine carboxylic acid A-127722 has been disclosed as a potent and ET(A)-selective antagonist, and is currently undergoing clinical trials. In our efforts to find antagonists with altered selectivity (ET(A)-selective, ET(B)-selective, or nonselective), we investigated the SAR of the 2-substituent on the pyrrolidine. Compounds with alkyl groups at the 2-position possessed ET(A) selectivity improved over A-127722 (1400-fold selective), with the best of these compounds showing nearly 19,000-fold selectivity. Copyright (C) 1999 Elsevier Science Ltd.
- Boyd, Steven A.,Mantei, Robert A.,Tasker, Andrew S.,Liu, Gang,Sorensen, Bryan K.,Henry Jr., Kenneth J.,Von Geldern, Thomas W.,Winn, Martin,Wu-Wong, Jinshyun R.,Chiou, William J.,Dixon, Douglas B.,Hutchins, Charles W.,Marsh, Kennan C.,Nguyen, Bach,Opgenorth, Terry J.
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p. 991 - 1002
(2007/10/03)
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- Solid-phase synthesis of pyrrolo[3,4-b]pyridines and related pyridine- fused heterocycles
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Sequential Hantzsch condensation and cyclative cleavage reactions have been used to define a novel solid-phase route to pyrrolo[3,4-b]pyridines and related pyridine-fused heterocycles. A combinatorial library of ~5000 compounds prepared via this chemistry is described.
- Bhandari, Ashok,Li, Bei,Gallop, Mark A.
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p. 1951 - 1960
(2007/10/03)
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- Simple and high yielding syntheses of β-keto esters catalysed by zeolites
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Simple and high yielding syntheses of several β-keto esters, catalysed by zeolite Hβ are reported. The methods developed include condensation of aldehydes with ethyl diazoacetate and transesterification of β-keto esters with primary, secondary, allylic and benzylic alcohols etc., all catalysed by Hβ. It was further observed that under microwave irradiation the yields of many aromatic β-keto esters were enhanced appreciably.
- Balaji,Chanda, Bhanu M.
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p. 13237 - 13252
(2007/10/03)
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- A novel convenient route to the naturally occurring 3-oxoacyl-L-homoserinelactones and related bacterial autoinducers
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The naturally occurring 3-oxohexanoyl-L-homoserinelactone (1a), a bacterial autoinducer has been prepared in 47% overall yield by condensing stable 3-oxohexanoic acid (2), prepared by hydrolysis from the corresponding ester (3), with L-homoserinelactone using hydroxybenzotriazole (HOBT) and dicyclohexylcarbodiimide (DCC) in non-aqueous media.
- Dekhane, Mouloud,Douglas, Kenneth T.,Gilbert, Peter
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p. 1883 - 1884
(2007/10/03)
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- Benzopyranones, a method for producing them and uses therefor
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Novel 2H-1-benzopyran-2-ones (coumarin derivatives) of the general formula (I) are provided: STR1 wherein R1, R2, R3, R4, X and Y are defined as in the specification, and the addition compounds thereof with physiologically compatible acids, intermediates and methods for the preparation thereof. The coumarin compounds possess a neuroprotective and anti-allergic action.
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- PYRAZOLOPYRIMIDINE DERIVATIVES WHICH ARE ANGIOTENSIN II RECEPTOR ANTAGONISTS
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The present invention relates to the derivatives of the formula STR1 and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment and prevention of cardiovascular diseases and in particular for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall, especially atherosclerosis.
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- TRIAZOLOPYRIMIDINE DERIVATIVES WHICH ARE ANGIOTENSIN II RECEPTOR ANTAGONISTS, THEIR METHODS OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS IN WHICH THEY ARE PRESENT
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The present invention relates to the derivatives of the formula STR1 and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment and prevention of cardiovascular diseases and in particular for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall, especially atherosclerosis.
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- TRIAZOLOPYRIMIDINE DERIVATIVES WHICH ARE ANGIOTENSIN II RECEPTOR ANTAGONISTS
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The present invention relates to the derivatives of formula: STR1 and to their tautomeric forms as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.
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- A safe, economical method for the preparation of β-oxo esters
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A high yield, economical method for preparation of β-oxo esters has been developed involving the reaction of acid chlorides with potassium ethyl malonate using a magnesium chloride-triethylamine base system in either acetonitrile or ethyl acetate solvents. The method is suitable for the preparation of high purity β-oxo esters in the laboratory and also in large scale production.
- Clay,Collom,Karrick,Wemple
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p. 290 - 292
(2007/10/02)
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- Triazolopyrimidine derivatives which are angiotensin II receptor antagonists processes for preparing them and pharmaceutical compositions containing them
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The present invention relates to the derivatives of formula: STR1 as well as to their addition salts and to their use in therapy, in particular for the treatment of cardiovascular diseases, especially for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.
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- Triazolopyrimidines which are angiotensin II receptor antagonists and pharmaceutical compositions in which they are present
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The present invention relates to the derivatives of the formula STR1 and their tautomeric forms, as well as their addition salts, and to their use in therapeutics, especially for the treatment of cardiovascular diseases and in particular for the treatment of hypertension, cardiac insufficiency and diseases of the arterial wall.
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- Synthesis of Mammea Coumarins. Part 1. The Coumarins of the Mammea A, B, and C Series
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The naturally-occuring Mammea coumarins of the 4-phenyl-(mammea A), propyl-(mammea B), and 4-pentyl-(mammea C) series have been prepared by Pechmann condensation of an acylphloroglucinol (3-methylbutyryl-, 2-methylbutyryl-, butyryl-, or 2-methylpropionyl-) with the appropriate β-ketoester to give a mixture of 6- and 8-acyl-5,7-dihydroxycoumarins that could be separated.C-Alkylation with 3-methylbut-2-enyl bromide, or 3,7-dimethylocta-2,6-dienyl chloride, in aqueous potassium hydroxide completed the synthesis of the Mammea coumarins having unmodified prenyl or geranyl substituents; oxidative modification of the prenyl group led to the mammea cyclo E and cyclo F coumarins.Some mammea cyclo D (chromeno) coumarins were synthesized by reaction of acylcoumarins with 1,1-dimethoxy-3-methylbutan-3-ol.
- Crombie, Leslie,Jones, Raymond C. F.,Palmer, Christopher J.
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p. 317 - 332
(2007/10/02)
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- Synthesis and Liquid Crystalline Phases of Pyridazine Derivatives I
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Seven pyridazine compounds were synthesized.The compounds have a general structure R-X-Y-PZ-R', where PZ is 3,6 disubstituted pyridazine ring, X and Y are either trans cyclohexyl or phenyl rings, R and R' are n-alkyl groups.The structure assignments were confirmed by carbon 13 nmr.Their liqiuid crystalline properties were evaluated.All of them have mesophases with a broad temperature range.
- Liang, Jason C.,Cross, Julie O.
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p. 123 - 130
(2007/10/02)
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- Sulfur-Extrusive Rearrangement of α-Acylthio Ester by Lithium Amide
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α-Acylthio esters readily undergo facile rearrangement to give β-keto esters on treatment with lithium amide at -78 deg C.Thiolactone 3, a key intermediate for thiolactonic antibiotics, was synthesized by utilizing the rearrangement.
- Tsuzuki, Kazuo,Akeyoshi, Masaharu,Omura, Satoshi
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p. 395 - 396
(2007/10/02)
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- Method of treating gastric ulcers using 5,6-dihydro-1,4-dithiinoxides
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5,6-Dihydro-1,4-dithiinoxides, compositions containing the 5,6-dihydro-1,4-dithiinoxides as their active ingredient and methods useful in the treatment of gastric ulcers are disclosed.
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- 1,4-Dihydropyridine esters
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A new class of 1,4-dihydropyridines which are characterized by the presence of ester substitutes at positions 3 and 5 of the nucleus and by the presence of an alkoxyalkyl at position 2. The products exhibit coronary activity and have particular application as coronary dilators, antifibrillators, anti-hypertensives, and as muscular and vascular spasmolytics.
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