- Having a spiro ring substituent of aryl morpholine compound, its preparation and use
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The invention discloses arylmorpholine compounds with spiro substituents. The arylmorpholine compounds are compounds having the following general formula (I), wherein X is N or CH; R1 is hydrogen, hydroxyl, alkoxy, halogen, amino, amido, acylamino, sulfam
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Paragraph 0143-0145
(2017/08/02)
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- An efficient method for the synthesis of 2′,3′-nonsubstituted cycloalkane-1,3-dione-2-spirocyclopropanes using (2-bromoethyl)-diphenylsulfonium trifluoromethanesulfonate
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An efficient and practical synthesis of 2′,3′-nonsubstituted cyclohexane-1,3-dione-2-spirocyclopropanes using a sulfonium salt was achieved. The reaction of 1,3-cyclohexanediones and (2-bromoethyl)diphenylsulfonium trifluoromethanesulfonate with powdered K2CO3 in EtOAc at room temperature (r.t.) provided the corresponding spirocyclopropanes in high yields. The synthetic method was also applied to 1,3-cyclopentanedione, 1,3-cycloheptanedione, 1,3-indanedione, acyclic 1,3-diones, ethyl acetoacetate, and Meldrum's acid.
- Nambu, Hisanori,Ono, Naoki,Hirota, Wataru,Fukumoto, Masahiro,Yakura, Takayuki
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p. 1763 - 1768
(2016/12/09)
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- AMINO ESTER DERIVATIVES, SALTS THEREOF AND METHODS OF USE
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The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Paragraph 0368
(2016/08/17)
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- Hydroxypurine compound and use thereof
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The invention discloses a hydroxypurine compound and a use of the hydroxypurine compound as a PDE2 or TNFa inhibitor and concretely discloses a compound shown in the formula (I) and its tautomer or pharmaceutically acceptable salt.
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Paragraph 0099; 0100; 0101; 0102
(2016/10/08)
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- Preparation method for efficiently synthesizing Sitafloxacin midbody (7S)-5-azaspiro[2.4] heptanes-7-phenylbutane
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The invention discloses a preparation method for efficiently synthesizing Sitafloxacin midbody (7S)-5-azaspiro[2.4] heptanes-7-phenylbutane. The method comprises the following steps that a first material shown as the accompanying drawing takes a reaction to obtain a second material shown as the accompanying drawing; the second material takes a reaction to obtain a third material shown as the accompanying drawing; the third material takes a reaction to obtain a fourth material shown as the accompanying drawing; the fourth material takes a reaction to obtain a fifth material shown as the accompanying drawing. The preparation method has the advantages that the single compound with a high ee value can be obtained; the unnecessary waste of materials is avoided; the yield is obviously improved; the operation is simple; the industrial application is easy; the production cost is reduced.
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Paragraph 0048; 0049
(2017/02/17)
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- COMBINATIONS OF HEPATITIS C VIRUS INHIBITORS
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The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
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Page/Page column 638
(2015/02/02)
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- Synthesis of (S)-7-amino-5-azaspiro[2.4]heptane via highly enantioselective hydrogenation of protected ethyl 1-(2-aminoaceto)cyclopropanecarboxylates
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Highly effective asymmetric hydrogenation of protected ethyl 1-(2-aminoaceto)cyclopropane carboxylates in the presence of [RuCl(benzene)(S)-SunPhos]Cl was realized, and high enantioselectivities (up to 98.7% ee) were obtained. This asymmetric hydrogenation provides a key intermediate for the enantioselective synthesis of (S)-7-amino-5-azaspiro[2.4] heptane moiety of quinolone antibacterial agents.
- Yao, Ying,Fan, Weizheng,Li, Wanfang,Ma, Xin,Zhu, Lvfeng,Xie, Xiaomin,Zhang, Zhaoguo
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experimental part
p. 2807 - 2813
(2011/06/19)
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- Synthesis of enantiomerically enriched α,α-disubstituted β,γ-epoxy esters using hydrolytic kinetic resolution catalyzed by salenCo(III)
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Novel α,α-disubstituted epoxy esters were prepared in enantiopure form by hydrolytic kinetic resolution (HKR) of the corresponding racemic mixtures using chiral salenCo(III) as catalyst. The methodology provides a convenient route to enantioenriched β,γ-epoxy esters 2a, 2c and 2d.
- Viera, Ignacio,Manta, Eduardo,Gonzalez, Lucia,Mahler, Graciela
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experimental part
p. 631 - 635
(2010/08/03)
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- AMINO ESTER DERIVATIVES, SAILTS THEREOF AND METHODS OF USE
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The present invention provides amino ester compounds, salts, and pharmaceutical formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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- COMPOUNDS AND METHODS OF USE
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The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
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Page/Page column 88
(2010/04/30)
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- BIS-PYRIDYLPYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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The invention provides novel bis-pyridylpyridones which are antagonists at the melanin-concentrating hormone receptor 1 (MCHR1 ), pharmaceutical compositions containing them, processes for their preparation, and their use in therapy and for the treatment
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Page/Page column 24-25
(2010/12/29)
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- Synthesis of (2-arylethylidene)cyclobutanes by palladium-catalyzed reactions of aryl halides with homoallyl alcohols bearing a trimethylene group at the allylic position
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Treatment of aryl bromides with homoallyl alcohols bearing a trimethylene group at the allylic position in the presence of cesium carbonate under palladium catalysis affords (2-arylethylidene) cyclobutanes selectively. The selective formation of the alkylidenecyclobutane skeleton results from regiospecific retroallylation of the homoallyl alcohols, which accompanies the transposition of the double bonds. Georg Thieme Verlag Stuttgart.
- Iwasaki, Masayuki,Yorimitsu, Hideki,Oshima, Koichiro
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supporting information; experimental part
p. 2177 - 2179
(2011/03/20)
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- PEPTIDE DEFORMYLASE INHIBITORS
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The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I), wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.
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Page/Page column 165, 177
(2009/06/27)
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- Imidazolium salts as phase transfer catalysts for the dialkylation and cycloalkylation of active methylene compounds
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The efficient synthesis of 1,1-disubstituted derivatives and the construction of cyclopropane and cyclopentane ring systems via dialkylation and cycloalkylation reactions of active methylene compounds using imidazolium salts as phase transfer catalyst is described. The dialkylation and cycloalkylation reactions of active methylene compounds in the presence of readily available imidazolium salts (ionic liquids) as phase transfer catalysts were performed to afford the respective dialkylated or cycloalkylated products. This method is very efficient for the synthesis of 1,1-disubstituted derivatives and cyclopropane and cyclopentane ring systems in a facile manner.
- Muthusamy, Sengodagounder,Gnanaprakasam, Boopathy
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p. 635 - 638
(2007/10/03)
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- Intramolecular heck couplings and cycloisomerizations of bromodienes and enynes with 1′,1′-disubstituted methylenecyclopropane terminators: Efficient syntheses of [3]dendralenes
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2-Bromoalka-1,n-dienes such as 9, 30 and 14 (n = 7) with tetrasubstituted methylenecyclopropane end groups, under palladium catalysis, underwent cyclization with cyclopropane-ring opening to give 2-ethenyl-3-methylene-1- cycloalkenes 41 (n = 6), 42 (n = 7
- Braese, Stefan,Wertal, Hanno,Frank, Daniel,Vidovic, Denis,De Meijere, Armin
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p. 4167 - 4178
(2007/10/03)
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- Microwave assisted phase transfer catalysis: An efficient solvent free method for the synthesis of cyclopropane derivatives
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Microwave assisted solvent free synthesis of cyclopropane derivatives 2a-e starting from active methylene compounds 1a-e and 1,2-dibromoethane under phase transfer conditions is described.
- Gumaste,Khan, Asgar J.,Bhawal,Deshmukh
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p. 420 - 422
(2007/10/03)
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- Process for producing 1-acyl-1-cyclopropanecarboxylate derivatives
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A process includes allowing a β-ketoester derivative represented by following Formula (1): wherein R1 is a hydrogen atom or a hydrocarbon group; and R2 is a hydrocarbon group, to react with 1,2-dichloroethane and there by produces a 1-acyl-1-cyclopropanecarboxylate derivative represented by following Formula (2): wherein R1 and R2 have the same meanings as defined above.
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- Substituted aminocycloalkylpyrrolidine derivatives and cis-substituted aminocycloalkylpyrrolidine derivatives
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An antimicrobial drug having excellent antimicrobial activity and high safety is disclosed, which comprises as an active ingredient, a quinolone-derivative having a substituted aminocycloalkylpyrrolidine as a substituent and which is further substituted w
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- Pyridonecarboxylic acid derivatives substituted by a bicyclic amino group as antibacterials
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This invention relates to a N1 -(halogenocyclopropyl)-substituted pyridonecarboxylic acid derivative represented by the following formula (I): STR1 wherein X1 is a halogen atom or a hydrogen atom; X2 is a halogen atom; R1 is a hydrogen atom, a hydroxyl group, a thiol group, a halogenomethyl group, an amino group, an alkyl group or an alkoxy group which may have a substituent group; R2 is a group represented by the following formula (II): STR2 wherein R3 and R4 are independently a hydrogen atom or an alkyl group and n is an integer of 1 or 2; A is a nitrogen atom or a partial structure of the following formula (III): STR3 wherein X3 is a hydrogen atom, a halogen atom, a cyano group, an amino group, an alkyl group, a halogenomethyl group, an alkoxyl group or a halogenomethoxyl group which may have a substituent group; and R is a hydrogen atom, a phenyl group, an acetoxymethyl group, a pivaloyloxymethyl group, an ethoxycarbonyl group, a choline group, a dimethylaminoethyl group, a 5-indanyl group, a phthalidynyl group, a 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl group, a 3-acetoxy-2-oxobutyl group, an alkyl group, an alkoxymethyl group or a phenylalkyl group, and provides a heterocyclic compound useful as antibacterial drugs.
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- Pyridonecarboxylic acid derivatives
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Quinolone derivatives are known as synthetic antimicrobial agents having a condensed pyridonecarboxylic acid skeleton, and those having substituents on various replaceable positions of said skeleton are known. In particular, if diastereomers exist, there are 4 or more kinds of stereoisomers. A mixture of diastereomers is a mixture of isomers having different physical properties and is difficult to apply as a drug as such. The present invention provides an antimicrobial 1-(1,2-cis-2-fluorocyclopropyl)-substituted quinolone derivative represented by formula I shown below which, although involving diastereomers, consists of a single stereoisomer. STR1 wherein R1 represents a methyl group, a difluoromethyl group, etc.; R2 represents a saturated nitrogen-containing heterocyclic group; A represents C--X3 or a nitrogen atom; X1 and X2 each represents a halogen atom; and X3 and Z represent a hydrogen atom, etc.
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- Optically active pyridonecarboxylic acid derivatives
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N1 -(1,2-cis-2-halogenocyclopropyl)-substituted pyridonecarboxylic acid derivatives represented by the following formula (I) the terms of which are defined in the specification and the salts thereof are disclosed: STR1 These compounds have pate
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- Electrosynthesis of cyclopropane derivatives by a Perkin-type reaction
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Electrolysis of active methylene compounds at a Pt cathode in MeCN in the presence of vicinal dihaloalkanes leads to cyclopropane derivatives in yields up to 90percent.In the cases of CH-acids with low pKa it is expedient to apply more active dihaloalkanes, while for CH-acids with higher pKa the desired product yields may be raised using electrogenerated bases. - Key words: CH-acids; 1,2-dihaloalkanes; cyclopropanes; electrosynthesis; electroreduction; electronegative bases; azobenzene.
- Petrosyan, V. A.,Vasil'ev, A. A.,Tatarinova, V. I.
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- Spiro compound
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The present invention relates to spiro compounds of general formula I: STR1 wherein the substituents are herein below defined. The present invention relates to antibacterial spiro compounds which are of value as drugs for humans, veterinary drugs or drugs for use in fish culture or as preservatives, and to antibacterial compositions containing one or more of the same compounds as active ingredients.
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- 24-cyclopropane vitamin D derivatives
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Vitamin D2 analogs in which a cyclopropane ring is introduced onto the 24-carbon of the side chain of 1α,25-dihydroxyvitamin D2 and 1α-hydroxyvitamin D2. The compounds are characterized by a marked intestinal calcium transport activity while exhibiting much lower activity than 1α,25-dihydroxy-vitamin D3 in their ability to mobilize calcium from bone. Because of their preferential calcemic activity, these compounds would be useful for the treatment of diseases where bone formation is desirbed, such as osteoporosis.
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- CATHODIC SYNTHESIS OF CYCLOPROPANE DERIVATIVES BY THE ELECTROLYSIS OF COMPOUNDS WITH AN ACTIVATED METHYLENE GROUP IN 1,2-DICHLOROETHANE
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The cathodic electrolysis of compounds with an activated methylene group in 1,2-dichloroethane leads to 1,1-disubstituted cyclopropanes.The current yield of these cyclopropane derivatives depends on the CH-acidity of the starting compounds and has a maximum at pKa ca.13.
- Vasil'ev, A. A.,Tatarinova, V. I.,Petrosyan, V. A.
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p. 631 - 633
(2007/10/02)
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- Synthesis of Averufin and its Role in Aflatoxin B1 Biosynthesis
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Described are two total syntheses of (+/-)-averufin (4) proceeding through a common intermediate and predicated on the efficient introduction of isotopic label(s) at side-chain and nuclear sites for the purpose of biosynthetic investigations of aflatoxin B1 (8).Using these methods, (+/-)--and --averufin, (65) and (68) respectively, and a 1:1 mixture of (+/-)-- and --averufin (71) were prepared and incorporated into aflatoxin B1 using mycelial suspensions of Aspergillus parasiticus (SU-1).In each instance efficient and specific utilization of label was observed in the product by (13)C-n.m.r.spectroscopy, demonstrating the intact incorporation of averufin.When compared with earlier observations of acetate incorporation, a complete correlation of the carbon skeleton from the intermediate anthraquinone stage of the four carbons lost in this overall process were unambiguously identified.In the formation of the dihydrobisfuran, the anthraquinone nucleus migrates to C-2' to branch the linear side-chain of averufin.Deuterium bound at C-1' in averufin is carried to C-13 of aflatoxin.Preparation from (+/-)-averufin (68) of (+/-)--averufin (73) and incorporation of the latter into versiconal acetate (5) demonstrated loss of the terminal two carbons of the averufin side-chain, presumably as acetate, by way of a Baeyer-Villiger-like oxidation.
- Townsend, Craig A.,Christensen, Siegfried B.,Davis, Steven G.
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p. 839 - 862
(2007/10/02)
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- Preparation and Cleavage of Some Cyclopropane Derivatives
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Alkylation of active methylene compounds with 1,2-dibromoethane using anhyd.K2CO3/DMF at room temperature gives cyclopropane derivatives which undergo selective transformation by simple methods.Cyclopropanes, obtained by the condensation of α-diazoacetophenones with olefins, are cleaved to trisubstituted olefins with Grignard reagent.Hydration of the products has also been studied.
- Podder, Ranjan Kumar,Sarkar, Ranjit Kumar,Ray, Suvas C.
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p. 530 - 536
(2007/10/02)
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- Perkin-Markovnikov Type Reaction Initiated with Electrogenerated Superoxide Ion
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The cyclic condensation of α,ω-dihaloalkanes with acticvated methylene of malonic acid and acetoacetic acid esters is studied using an electrogenerated superoxide ion.Two possible mechanisms for this reaction are postulated.
- Ojima, Fumihiro,Matsue, Tomokazu,Osa, Tetsuo
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p. 2235 - 2238
(2007/10/02)
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- CYCLOALKYLATION BY THE α,ω-DIBROMIDES OF COMPOUNDS CONTAINING AN ACTIVATED METHYLENE GROUP AS A METHOD FOR THE SYNTHESIS OF 1,1-DISUBSTITUTED CYCLOALKENES
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A convenient preparative method was developed for the cycloalkylation of active methylene compounds, including β-diketones, by the dibromides BrCH2(CH2)nCH2Br (n = 0,1,2) in the presence of an excess of potassium carbonate in DMSO.The reaction gives high yields for the dibromides with n = 0 and 2, whereas the formation of cyclobutanes (n=1) is complicated by O,C-alkylation.The 1-substituted 1-acylcyclopropanes undergo thermal isomerization to the corresponding dihydrofuranes.
- Zefirov, N. S.,Kuznetsova, T. S.,Kozhushkov, S. I.,Surmina, L. S.,Rashchupkina, Z. A.
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p. 474 - 480
(2007/10/02)
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- OPENING OF THE THREE-MEMBERED RING IN 1,1-DISUBSTITUTED CYCLOPROPANES AS A METHOD FOR THE SYNTHESIS OF FUNCTIONAL DERIVATIVES OF PYRAZOLE AND ISOXAZOLE
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The reaction of 1,1-diacylcyclopropanes with hydrazine and hydroxylamine derivatives, which leads to nucleophilic opening of the three-membered ring and the formation of pyrazole and isoxazole derivatives, was studied.The dependence of the occurrence of t
- Zefirov, N. S.,Kozhushkov, S. I.,Kuznetsova, T. S.
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p. 644 - 650
(2007/10/02)
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