- 4-hydroxy-2-quinolones. 95. Synthesis, structure, and antitubercular properties of hetarylamides of 4-hydroxy-2-oxo-1,2,5,6,7,8-hexahydroquinoline-3- carboxylic acid
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The optimal conditions for obtaining hetarylamides of 4-hydroxy-2-oxo-1,2, 5,6,7,8-hexahydroquinoline-3-carboxylic acid are suggested on the basis of derivatographic investigations. The 1H NMR spectra of the synthesized compounds, their spatial
- Ukrainets,Kolesnik,Sidorenko,Gorokhova,Turov
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- Synthesis and evaluation of (E)-2-(acrylamido)cyclohex-1-enecarboxylic acid derivatives as HCA1, HCA2, and HCA3 receptor agonists
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2-(3-(Naphthalen-2-yl)propanamido)cyclohex-1-enecarboxylic acid and its 6-hydroxynaphthalen-2-yl analogue are well-known hydroxyl-carboxylic acid (HCA) receptor HCA2 agonists. A series of novel aryl derivatives of 2-amidocyclohex-1-ene carboxylic acid tha
- Bobileva, Olga,Bokaldere, Rasma,Gailite, Vija,Kaula, Ilze,Ikaunieks, Martins,Duburs, Gunars,Petrovska, Ramona,Mandrika, Ilona,Klovins, Janis,Loza, Einars
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p. 3654 - 3669
(2014/07/07)
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- Synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols or 3-amino alcohols using iodobenzene dichloride and sodium azide
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A general and efficient method for the synthesis of oxazolidin-2-ones and imidazolidin-2-ones directly from 1,3-diols and 3-amino alcohols has been developed using the same reagent combination of iodobenzene dichloride (PhICl2) and sodium azide (NaN3).
- He, Tian,Gao, Wen-Chao,Wang, Wei-Kun,Zhang, Chi
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supporting information
p. 1113 - 1118
(2014/04/03)
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- PYRIDINE DERIVATIVES AS MICROBIOCIDES
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Compounds of formula (I) wherein the other substituents R1, R2, R3, and G are as defined in claim 1, and their use as microbiocides.
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Page/Page column 60
(2013/03/26)
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- An unusual boron tribromide-mediated, one-pot bromination/cyclization reaction. Application to the synthesis of a highly strained cyclopenta[1,3] cyclopropa[1,2-b]pyrrolizin-8-one
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Performing Jefford's cyclization of ethyl 2-pyrrol-1-ylcyclohex-2-ene-1- carboxylate (5) using boron tribromide in refluxing dichloromethane led to a trans-cis bromopyrrolohydrindolone 7 whose debromination in alkaline medium afforded a highly strained cy
- Jourdan, Jean-Pierre,Rochais, Christophe,Legay, Remi,Sopkova De Oliveira Santos, Jana,Dallemagne, Patrick
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p. 1133 - 1136
(2013/03/14)
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- Tandem transformations of nitriles into N-heterocyclic compounds by electrophilic trapping of Blaise reaction intermediates
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Tandem transformations of nitriles into various N-heterocycles have been accomplished through the reaction of electrophiles with Blaise reaction intermediates formed in situ. The reaction of the Blaise reaction intermediates with propiolates gives 2-pyridones through consecutive C- and N-nucleophilic reactions. The tandem reactions of the Blaise reaction intermediate with 1,3-enynes proceed through C-nucleophilic addition followed by an electrocyclization-aromatization cascade to give pyridines. Exocyclic enamino esters can be prepared by transformations of ω-chloroalkyl nitriles through chemoselective intramolecular alkylation of the Blaise reaction intermediate. Palladium-catalyzed intramolecular arylations or copper-catalyzed intermolecular cross-coupling reactions of the Blaise reaction intermediate give a range of indole derivatives. Combinations of tandem alkylations and palladium-catalyzed couplings of the Blaise reaction intermediates of ω-chloroalkyl nitriles give N-fused indoles. Georg Thieme Verlag Stuttgart · New York.
- Kim, Juhyun,Chun, Yusung,Shin, Hyunik,Lee, Sang-Gi
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experimental part
p. 1809 - 1817
(2012/08/08)
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- Chemoselective intramolecular alkylation of the Blaise reaction intermediates: Tandem one-pot synthesis of exo -cyclic enaminoesters and their applications toward the synthesis of N -heterocyclic compounds
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The intramolecular alkylative reactivity and N/C selectivity of the various Blaise reaction intermediates, which are formed from the reaction of the Reformatsky reagents with ω-chloroalkyl nitriles, did not reach the synthetic potential as an entry to exo-cyclic enaminoesters. To circumvent this issue, various additives were investigated, among which the addition of NaHMDS dramatically enhanced the reactivity and N/C selectivity. This modification provided a highly efficient route for the synthesis of various N-fused heterocyclic compounds, as it requires only two steps from nitriles.
- Kim, Ju Hyun,Shin, Hyunik,Lee, Sang-Gi
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experimental part
p. 1560 - 1565
(2012/04/04)
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- Discovery of the investigational drug TAK-441, a pyrrolo[3,2-c]pyridine derivative, as a highly potent and orally active hedgehog signaling inhibitor: Modification of the core skeleton for improved solubility
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We recently reported the discovery of the novel pyrrolo[3,2-c]quinoline-4- one derivative 1 as a potent inhibitor of Hedgehog (Hh) pathway signaling. However, the PK evaluation of 1 at high dosage (100 mg/kg) revealed the C max value 3.63 μg/mL
- Ohashi, Tomohiro,Oguro, Yuya,Tanaka, Toshio,Shiokawa, Zenyu,Tanaka, Yuta,Shibata, Sachio,Sato, Yoshihiko,Yamakawa, Hiroko,Hattori, Harumi,Yamamoto, Yukiko,Kondo, Shigeru,Miyamoto, Maki,Nishihara, Mitsuhiro,Ishimura, Yoshimasa,Tojo, Hideaki,Baba, Atsuo,Sasaki, Satoshi
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p. 5507 - 5517
(2012/10/30)
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- PYRIMIDINE DERIVATIVE
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This invention provides pyrimidine derivatives represented by a formula, in the formula, ring A stands for carbocyclic group or heterocyclic group, X 1 stands for hydrogen, lower alkyl, amino, etc., X 2 stands for hydrogen or lower alkyl, Y stands for a direct bond or sulfur or nitrogen, n stands for an integer of 0 - 4, and Ar stands for a group of the following formula, or a salt thereof, which concurrently exhibit 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity and are useful for therapy and treatments of diseases such as IBS. The invention furthermore provides a therapeutic method of IBS, characterized by having 5-HT 1A agonistic activity and 5-HT 3 antagonistic activity work simultaneously and cooperatively in vivo, which comprises either administering 5-HT 3 antagonistic agent which concurrently exhibits 5-HT 1A agonistic activity, or administering 5-HT 1A agonistic agent and 5-HT 3 antagonistic agent simultaneously, in sequence or at an interval.
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Page/Page column 52; 68
(2010/11/24)
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- Efficient synthesis of β-amino-α,β-unsaturated carbonyl compounds
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A versatile and high-yielding procedure for the synthesis of β-enamino esters and β-enaminones is presented: in the presence of tetraethyl orthosilicate, a number of highly functional β-enamino esters were obtained; this method provided an alternative for the formation of β-amino-α,β-unsaturated carbonyl compounds with mild and functional group compatible reaction conditions. The Royal Society of Chemistry and the Centre National de la Recherche Scientifique 2005.
- Zhao, Yuanhong,Zhao, Jingfeng,Zhou, Yongyun,Lei, Ze,Li, Liang,Zhang, Hongbin
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p. 769 - 772
(2007/10/03)
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- Enantioselective hydrogenation of tetrasubstituted olefins of cyclic β-(acylamino)acrylates
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Hydrogenation of a series of cyclic β-(acylamino)acrylates with tetrasubstituted olefins has been accomplished successfully with the use of Ru catalysts with chiral biaryl ligands such as C3-TunaPhos, and up to over 99% ee's have been achieved. This methodology provides an efficient catalytic method for the synthesis of both cis and trans chiral cyclic β-amino acid derivatives. Copyright
- Tang, Wenjun,Wu, Shulin,Zhang, Xumu
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p. 9570 - 9571
(2007/10/03)
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- Stereochemistry and mechanism of the chemoselective allylation of α-substituted β-keto esters with allyl bromide mediated by Zn in NH4Cl(aq)-THF
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Six α-substituted β-keto esters were chemoselectively alfylated at the keto group by a Zn-mediated reaction with allyl bromide in NH4Cl(aq)-THF. The reactions gave diastereomeric homoallylic alcohols with d.e.s ranging from 28 to 74%. With ethyl 2-chloroacetoacetate, substitution of the chlorine atom by the allyl group took place. Similarly, on allylation of diethyl benzoylmalonate, diethyl malonate was eliminated. These reactions support a radical mechanism. The relative configurations of the formed diastereomers were determined by a combination of 1H NMR spectroscopy and molecular modeling. The stereochemistry of the diastereomers supports a mechanism including strong association of the keto ester with the metal surface. Acta Chemica Scandinavica 1997.
- Ahonen, Matthias,Sjoeholm, Rainer
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p. 785 - 790
(2007/10/03)
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