- Expeditious and practical synthesis of tertiary alcohols from esters enabled by highly polarized organometallic compounds under aerobic conditions in Deep Eutectic Solvents or bulk water
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An efficient protocol was developed for the synthesis of tertiary alcohols via nucleophilic addition of organometallic compounds of s-block elements (Grignard and organolithium reagents) to esters performed in the biodegradable choline chloride/urea eutectic mixture or in water. This approach displays a broad substrate scope, with the addition reaction proceeding quickly (20 s reaction time) and cleanly, at ambient temperature and under air, straightforwardly furnishing the expected tertiary alcohols in yields of up to 98%. The practicability of the method is exemplified by the sustainable synthesis of some representative S-trityl-L-cysteine derivatives, which are a potent class of Eg5 inhibitors, also via telescoped one-pot processes.
- Quivelli, Andrea F.,D'Addato, Giovanna,Vitale, Paola,García-álvarez, Joaquín,Perna, Filippo M.,Capriati, Vito
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- Rhodium(III)-Catalyzed Oxidative Intramolecular 1,1-Oxyamination of Alkenes with Protected Amino Acids to Produce Oxazoloisoindole-2,5-diones
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It has been established that an electron-deficient bis(ethoxycarbonyl)-substituted cyclopentadienyl (CpE) rhodium(III) complex catalyzes the oxidative intramolecular 1,1-oxyamination of alkenes with N-benzoyl amino acids to produce oxazoloisoindole-2,5-diones. Experimental and theoretical mechanistic studies revealed that this oxidative 1,1-oxyamination proceeds via not the aza-Wacker reaction but the formation of a rhoda(III)oxazolidine initiated by the carboxylic acid-directed N?H bond cleavage.
- Takahashi, Hiroto,Nagashima, Yuki,Tanaka, Ken
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supporting information
p. 1891 - 1895
(2021/04/05)
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- Evaluation of novel N′-(3-hydroxybenzoyl)-2-oxo-2H-chromene-3-carbohydrazide derivatives as potential HIV-1 integrase inhibitors
-
In an attempt to identify potential new agents that are active against HIV-1 IN, a series of novel coumarin-3-carbohydrazide derivatives were designed and synthesised. The toxicity profiles of these compounds showed that they were non-toxic to human cells and they exhibited promising anti-HIV-1 IN activities with IC50 values in nM range. Also, an accompanying molecular modeling study showed that the compounds bind to the active pocket of the enzyme.
- Jesumoroti, Omobolanle J.,Faridoon,Mnkandhla, Dumisani,Isaacs, Michelle,Hoppe, Heinrich C.,Klein, Rosalyn
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- Microwave-Assisted Synthesis of Benzofuran-3(2H)-ones
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A new method for the synthesis of benzofuran-3(2H)-ones under microwave conditions was developed. The reaction conditions were screened, and the scope of benzoate substrates was investigated. The results showed that our method could provide rapid access to these important dihydrobenzofuranones in 43% to 58% yields.
- Hu, Xiaojing,Lai, Huimin,Zhao, Fangfei,Hu, Shuyu,Sun, Qianqian,Fang, Lizhen
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p. 745 - 750
(2019/10/14)
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- Gold promoted arylative cyclization of alkynoic acids with arenediazonium salts
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Alkynoic acids derived from salicylic acid and analogues undergo arylative cyclization with arenediazonium salts promoted by gold in the absence of external ligands. The reaction is thermally induced and proceeds even in the absence of light. A difference in regioselectivity has been found compared with that observed in the cycloisomerization process of the same type of compounds.
- Carrillo-Arcos, Ulises A.,Porcel, Susana
-
supporting information
p. 1837 - 1842
(2018/03/23)
-
- Vitamin Catalysis: Direct, Photocatalytic Synthesis of Benzocoumarins via (-)-Riboflavin-Mediated Electron Transfer
-
An operationally simple protocol is disclosed to facilitate entry to benzo-3,4-coumarins directly from biaryl carboxylic acids without the need for substrate prefunctionalization. Complementary to classic lactonization strategies, this disconnection relies on the oxidation competence of photoactivated (-)-riboflavin (vitamin B2) to generate the heterocyclic core via photoinduced single electron transfer. Collectively, the inexpensive nature of the catalyst, ease of execution, and absence of external metal additives are a convincing endorsement for the incorporation of simple vitamins in contemporary catalysis.
- Morack, Tobias,Metternich, Jan B.,Gilmour, Ryan
-
supporting information
p. 1316 - 1319
(2018/03/09)
-
- 11C- and 18F-Labeled Radioligands for P-Glycoprotein Imaging by Positron Emission Tomography
-
P-Glycoprotein (P-gp) is an efflux transporter widely expressed at the human blood-brain barrier. It is involved in xenobiotics efflux and in onset and progression of neurodegenerative disorders. For these reasons, there is great interest in the assessmen
- Cantore, Mariangela,Benadiba, Marcel,Elsinga, Philip H.,Kwizera, Chantal,Dierckx, Rudi A. J. O.,Colabufo, Nicola Antonio,Luurtsema, Gert
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p. 108 - 118
(2016/01/15)
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- Oxidative cyclization of alkenoic acids promoted by AgOAc
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Alkenoic acids derived from salicylic acid and analogues undergo an unexpected oxidative cyclization process triggered by AgOAc leading to 4H-benzo[d][1,3]dioxin-4-ones. The process is affected by the substitution on the aryl and the allyl units.
- Carrillo-Arcos, Ulises A.,Rojas-Ocampo, Jonathan,Porcel, Susana
-
supporting information
p. 479 - 483
(2016/01/09)
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- Computational and Experimental Studies of Phthaloyl Peroxide-Mediated Hydroxylation of Arenes Yield a More Reactive Derivative, 4,5-Dichlorophthaloyl Peroxide
-
The oxidation of arenes by the reagent phthaloyl peroxide provides a new method for the synthesis of phenols. A new, more reactive arene oxidizing reagent, 4,5-dichlorophthaloyl peroxide, computationally predicted and experimentally determined to possess enhanced reactivity, has expanded the scope of the reaction while maintaining a high level of tolerance for diverse functional groups. The reaction proceeds through a novel "reverse-rebound" mechanism with diradical intermediates. Mechanistic insight was achieved through isolation and characterization of minor byproducts, determination of linear free energy correlations, and computational analysis of substituent effects of arenes, each of which provided additional support for the reaction proceeding through the diradical pathway.
- Camelio, Andrew M.,Liang, Yong,Eliasen, Anders M.,Johnson, Trevor C.,Yuan, Changxia,Schuppe, Alex W.,Houk,Siegel, Dionicio
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p. 8084 - 8095
(2015/09/01)
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- CYCLIC PEROXIDE OXIDATION OF AROMATIC COMPOUND PRODUCTION AND USE THEREOF
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The present invention provides a method for converting an aromatic hydrocarbon to a phenol by providing an aromatic hydrocarbon comprising one or more aromatic C-H bonds and one or more activated C-H bonds in a solvent; adding a phthaloyl peroxide to the solvent; converting the phthaloyl peroxide to a di-radical; contacting the di-radical with the one or more aromatic C-H bonds; oxidizing selectively one of the one or more aromatic C-H bonds in preference to the one or more activated C-H bonds; adding a hydroxyl group to the one of the one or more aromatic C-H bonds to form one or more phenols; and purifying the one or more phenols.
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Page/Page column 10
(2014/10/15)
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- Palladium-catalyzed intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides
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Give me a ring? An efficient approach has been developed for the intramolecular decarboxylative coupling of arene carboxylic acids/esters with aryl bromides catalyzed by palladium (see scheme). From a synthetic viewpoint, this method is highly attractive because the catalyst loading is low, the optimized reaction conditions are mild, and the substrate scope is broad. Copyright
- Shen, Zengming,Ni, Zhenjie,Mo, Song,Wang, Jing,Zhu, Yamin
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supporting information; experimental part
p. 4859 - 4865
(2012/06/04)
-
- Deslongchamps annulations with benzoquinone monoketals
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The so-called Deslongchamps annulation of deprotonated γ, δ-unsaturated β-ketoesters 15 to 2-(alkoxycarbonyl)cyclohex-2-en-1- ones or similarly activated cyclohex-2-en-1-ones offers a versatile access to various kinds of decalindiones. The scope of Deslon
- Petrovic, Denis,Brueckner, Reinhard
-
supporting information; experimental part
p. 6524 - 6527
(2012/02/01)
-
- Synthesis, structural investigations, hydrogen-deuterium exchange studies, and molecular modeling of conformationally stablilized aromatic oligoamides
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Biasing the conformational preferences of aromatic oligoamides by internally placing intramolecular hydrogen bonds has led to a series of stably folded molecular strands. This article presents the results from extensive solid-state, solution, and computational studies on these folding oligomers. Depending on its backbone length, an oligoamide adopts a crescent or helical conformation. Surprisingly, despite the highly repetitive nature of the backbone, the internally placed, otherwise very similar intramolecular hydrogen bonds showed significantly different stabilities as demonstrated by hydrogen-deuterium exchange data. It was also observed that the hydrogen-bonding strength can be tuned by adjusting the substituents attached to the exterior of the aromatic backbones. Examining the amide hydrogen-deuterium exchange rates of trimers revealed that a six-membered hydrogen bond nearing the ester end is the weakest among all the four intramolecular hydrogen bonds of a molecule. This observation was verified by ab initio quantum mechanical calculations at the level of B3LYP/6-31G. Such a "weak point" creates the "battle of the bulge" where backbone twisting is centered, which is consistently observed in the solid-state structures of the four trimer molecules studied. In the solid state, the oligomers assemble into interesting one-dimensional structures. A pronounced columnar packing of short oligomers (i.e., dimers, trimers, and tetramer) and channel-like, potentially ion-conducting stacks of longer oligomers (i.e., tetramer, pentamer, and hexamer) were observed.
- Yan, Yan,Qin, Bo,Ren, Changliang,Yip, Yeow Kwan,Ye, Ruijuan,Zeng, Huaqiang,Chen, Xiuying,Su, Haibin,Zhang, Dawei
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supporting information; experimental part
p. 5869 - 5879
(2010/07/13)
-
- The first total synthesis of lactonamycin, a hexacyclic antitumor antibiotic
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The total synthesis of lactonamycin has been achieved. The synthesis includes sequential intramolecular conjugate addition of alcohols to the acetylenic ester, stereoselective glycosylation of the tertiary alcohol, and Michael-Dieckmann type cyclization w
- Tatsuta, Kuniaki,Tanaka, Hiroaki,Tsukagoshi, Hitomi,Kashima, Takafumi,Hosokawa, Seijiro
-
scheme or table
p. 5546 - 5549
(2010/11/03)
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- Leaving group assistance in the La3+-catalyzed cleavage of dimethyl (o-methoxycarbonyl)aryl phosphate triesters in methanol
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The catalytic methanolysis of a series of dimethyl aryl phosphate triesters where the aryl groups contain an o-methoxycarbonyl (o-CO2Me) substituent (4a-i) was studied at 25°C in methanol containing La 3+ at various concentrations and sspH. Determination of the second-order rate constant for La3+ 2-catalyzed cleavage of substrate 4a (dimethyl (o-methoxycarbonyl) phenyl phosphate) as a function of sspH was assessed in terms of a speciation diagram that showed that the process was catalyzed by La3+ 2(-OCH3)x dimers, where x = 1-5, that exhibit only a 5-fold difference in activity between all the species. The second-order catalytic rate constants (k2La) for the catalyzed methanolysis of 4a-i at sspH 8.7 fit a Bronsted relationship of log k2La= (-0.82 ± 0.11)sspKalg + (11.61 ± 1.48), where the gradient is shallower than that determined for a series of dimethyl aryl phosphates that do not contain the o-CO2Me substituent, log k2La = (-1.25 ± 0.06)s spKalg + (16.23 ± 0.75). Two main observations are that (1) the o-CO2Me group preferentially accelerates the cleavage of the phosphate triesters with poor leaving groups relative to those with good leaving groups and (2) it provides an increase in cleavage rate relative to those of comparable substrates that do not have that functional group, e.g., k2La(dimethyl o-(methoxycarbonyl) phenyl phosphate)/k2La(dimethyl phenyl phosphate) = 60. Activation parameters for the La3+2-catalyzed methanolysis of 4a and dimethyl 4-nitrophenyl phosphate show respective ΔH? (ΔS?) values of 3.3 kcal/mol (-47 cal/mol·K) and 0.7 kcal/mol (-46.5 cal/mol·K). The data are analyzed in terms of a concerted reaction where the catalytic complex (La3+2( -OCH3)x-1) binds to the three components of a rather loose transition state composed of a nucleophile CH3O -, a nucleofuge -OAr, and a central (RO)2P 2+-O- in a way that provides leaving group assistance to the departing aryloxy group.
- Edwards, David R.,Liu, C. Tony,Garrett, Graham E.,Neverov, Alexei A.,Brown, R. Stan
-
supporting information; experimental part
p. 13738 - 13748
(2010/01/06)
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- Dissociative solvolytic cleavage of methyl (ortho-Carboxymethyl)Aryl phosphate diesters mediated by Yb3+ in methanol gives a 10 12-fold rate acceleration attributable to leaving group assistance
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The Yb3+-catalyzed cleavage of a series of eight methyl aryl phosphates (2a-h) where the aryl groups all contain an ortho-methoxycarbonyl group was studied in acidic methanol from 1.34 ≤ spHs ≤ 3.34 at 25 °C. All substrates show saturation binding of the metal ion that is analyzed to provide a conditional binding constant (K)b for a 1:1 substrate/Yb3+ complex and catalytic rate constant (A cat) that varies between about 2 × 10-3 and 50 × 10-3 s-1 overthe range of substrates. Detailed analysis indicates that at very low c oncentration of Yb3+, 3 equiv of substrate are bound, and with increasing [Yb3+], the binding changes to a 1:1 complex which decomposes by a pathway independent of spHs over the range investigated. Control studies show that substrates without the o-methoxycarbonyl group still bind to the Yb 3+ with approximately the same strength as do the o-methoxycarbonyl containing substrates but have no observable reaction when bound. A Jaffe plot of the kcat vs substituent ?-values indicates that, during the catalyzed reactions of 2a-h, the phenoxy-O and C(O)OCH3 groups accommodate negative and positive charge respectively, the p phosphate and p c(o)OMe values being (1.84 ±0.11) and ( 0.85 ±0.14). For all these substrates, the final reaction products are dimethyl phosphate and the Yb3+ complex of the phenoxide. A study of the binding of the parent phenols to Yb3+ indicates that log(Kbind) = (0.84 ± 0.06)sspKa+ (3.4 ± 0.9), r2 = 0.9664 for phenols containing the o-methoxycarbonyl group; for those lacking that substituent log(Kb ind) = (0.96 ± 0.04)s spKa- (1.73 ± 0.4), (r2 = 0.99). For the catalyzed reacti on the βlg = -0.48, while the βeq = -0.95, leading to a Leffler parameter of α = 0.51. A mechanism is presented for the catalyzed reaction which is highly dissociative, having a transition state where the Yb3+ translocates during the cleavage reaction to assist the leaving group's departure with weak nucleophilic assistance by the solvent methanol. A comparison of the catalyzed rate of reaction with a computed rate of reaction attributable to solvent alone indicates that Yb3+ provides leaving group assistance on the order of 1012-fold, stabilizing the transition state for cleavage by some 16 kcal/mol.
- Edwards, David R.,Neverov, Alexei A.,Brown, R. Stan
-
supporting information; experimental part
p. 368 - 377
(2009/06/28)
-
- Synthesis and cannabinoid activity of a variety of 2,3-substituted 1-benzo[b]thiophen derivatives and 2,3-substituted benzofuran: Novel agonists for the CB1 receptor
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An exploratory chemical effort has been undertaken to develop a novel series of compounds as selective CB1 agonists. It is hoped that compounds of this type will have clinical utility in pain control and cerebral ischaemia following stroke or traumatic head injury. We report here medicinal chemistry studies directed towards the investigation of several classes of 1-benzo[b]thiophen and benzofuran derivatives as novel CB1 agonists. We have discovered a novel series of compounds, which contain a 1-benzo[b]thiophen or a benzofuran group as the central aromatic group. Our investigation of this series of compounds has enhanced our understanding of the importance of binding sites within the CB1 receptor for favourable CB1 potency. Our understanding of these factors allowed us to modify the structure of a 1-benzothiophen derivative and improve its potency at the CB1 receptor. CSIRO 2008.
- Moloney, Gerard P.,Angus, James A.,Robertson, Alan D.,Stoermer, Martin J.,Robinson, Michael,Lay, Lucy,Wright, Christine E.,McRae, Ken,Christopoulos, Arthur
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p. 484 - 499
(2008/12/20)
-
- Synthesis and structure activity relationship studies of benzothieno[3,2-b]furan derivatives as a novel class of IKKβ inhibitors
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As a novel class of IKKβ inhibitors, a series of tricyclic furan derivatives was designed and synthesized based on the structure of known thiophene IKKβ inhibitors. Among the various fused furan derivatives synthesized, a benzothieno[3,2-b]furan derivative 13a displayed potent inhibitory activity towards IKKβ in enzymatic and cellular assays. The potent inhibitory activity originates from an intramolecular non-bonded S...O interaction which was confirmed by the X-ray structure of JNK3 with 16k. The introduction of further substituents on the core structure led to the discovery of the 6-alkoxy derivatives, which possessed a comparable IKKβ inhibitory activity to 13a and an improved metabolic stability. Among these, appropriately lipophilic compounds 16a, h, i, and 13g (logD>2) were found to possess good oral bioavailability.
- Sugiyama, Hideyuki,Yoshida, Masato,Mori, Kouji,Kawamoto, Tomohiro,Sogabe, Satoshi,Takagi, Terufumi,Oki, Hideyuki,Tanaka, Toshimasa,Kimura, Hiroyuki,Ikeura, Yoshinori
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p. 613 - 624
(2008/02/13)
-
- Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum
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A parallel synthetic strategy to the 9-aminoacridine scaffold of the classical anti-malarial drug quinacrine (2) is presented. The method features a new route to 9-chloroacridines that utilizes triflates of salicylic acid derivatives, which are commercially available in a variety of substitution patterns. The route allows ready variation of the two diversity elements present in this class of molecules: the tricyclic aromatic heterocyclic core, and the disubstituted diamine sidechain. In this study, a library of 175 compounds was designed, although only 93 of the final products had purities acceptable for screening. Impurity was generally due to incomplete removal of 9-acridones (18), a degradation product of the 9-chloroacridine synthetic intermediates. The library was screened against two strains of Plasmodium falciparum, including a model of the drug-resistant parasite, and six novel compounds were found to have IC50 values in the low nanomolar range.
- Anderson, Marc O.,Sherrill, John,Madrid, Peter B.,Liou, Ally P.,Weisman, Jennifer L.,DeRisi, Joseph L.,Guy, R. Kiplin
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p. 334 - 343
(2007/10/03)
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- The discovery of fluoropyridine-based inhibitors of the Factor VIIa/TF complex
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The activated Factor VII/tissue factor complex (FVIIa/TF) plays a key role in the formation of blood clots. Inhibition of this complex may lead to new antithrombotic drugs. An X-ray crystal structure of a fluoropyridine-based FVIIa/TF inhibitor bound in the active site of the enzyme complex suggested that incorporation of substitution at the 5-position of the hydroxybenzoic acid side chain could lead to the formation of more potent inhibitors through interactions with the S1′/S2′ pocket.
- Kohrt, Jeffrey T.,Filipski, Kevin J.,Cody, Wayne L.,Cai, Cuiman,Dudley, Danette A.,Van Huis, Chad A.,Willardsen, J. Adam,Rapundalo, Stephen T.,Saiya-Cork, Kamlai,Leadley, Robert J.,Narasimhan, Lakshmi,Zhang, Erli,Whitlow, Marc,Adler, Marc,McLean, Kirk,Chou, Yuo-Ling,McKnight, Cecile,Arnaiz, Damian O.,Shaw, Kenneth J.,Light, David R.,Edmunds, Jeremy J.
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p. 4752 - 4756
(2007/10/03)
-
- Utilities of olefin derivatives
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Compounds having an activity to enhance the expression of apoAI are provided. Compounds of formula (I): in which Ar1 and Ar2 are independently a phenyl, naphthyl, or monocyclic or bicyclic aromatic heterocyclic group, which may be optionally substituted; —X— is —N═CZ2-, —CY2═CZ2-, —CY2Y3—CHZ2-, —S—, —O—, or the like; Y1, Y2, Y3, Z1 and Z2 are independently a hydrogen, a halogen, a lower alkyl, a phenyl, or the like; Z1 and Z2 may be independently a linker group that may combine with Ar2 and Ar1 to form a condensed ring; m is 0 or 1, and n is 0 to 2; a prodrug thereof, a pharmaceutically acceptable salt or solvate of them; are disclosed.
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Page/Page column 13
(2008/06/13)
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- Synthesis and structure-activity relationship study of lamellarin derivatives
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Ten derivatives (3-12) of marine alkaloid lamellarin D (1) were synthesized and evaluated for cytotoxicity against a HeLa cell line in an effort to examine their structure-activity relationships. It appeared that the hydroxyl groups at positions C-8 and C-20 of 1 were important structural requirements for cytotoxic activity, while the hydroxyl group at C-14 and the two methoxy groups at C-13 and C-21 were not necessary for the activity.
- Ishibashi, Fumito,Tanabe, Shinji,Oda, Tatsuya,Iwao, Masatomo
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p. 500 - 504
(2007/10/03)
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- Total synthesis and absolute configuration of riccardiphenols A and B, isolated from the Liverwort Riccardia crassa
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The title compounds were synthesized as optically active forms using chiral Michael addition of the imine, prepared from 2-methylcyclohexanone and (S)-(-)-phenylethylamine, to methyl propiolate. The etherification of the intermediate triol was accomplished by TsOH-catalyzed cyclization. The absolute configurations of the natural products, riccardiphenols A and B, were established as 1 and 2, respectively.
- Tori,Hamaguchi,Sagawa,Sono,Asakawa
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p. 5362 - 5370
(2007/10/03)
-
- 1,4-benzothiazepine derivatives
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An object of the invention is to provide compounds having a myocardial KD (Kinetic cell death)-inhibiting effect without being accompanied by a cardiodepressant effect. A 1,4-benzothiazepine derivative represented by the following Formula [I]: STR1 wherei
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- Zatosetron, a Potent, Selective, and Long-Acting 5HT3 Receptor Antagonist: Synthesis and Structure-Activity Relationships
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Antagonists of 5HT3 receptors are clinically effective in treating nausea and emesis associated with certain oncolytic drugs, including cisplatin.Moreover, these agents may be useful in pharmacological management of several central nervous system disorders, including anxiety, schizophrenia, dementia, and substance abuse.Our studies on aroyltropanamides led to the discovery that dihydrobenzofuranyl esters and amides are potent 5HT3 receptor antagonists.Simple benzoyl derivatives of tropine and 3α-aminotropane possessed weak 5HT3 receptor antagonist activity, as judged by blockade of bradycardia produced by iv injection of serotonin (5HT) to anesthetized rats.Within this series, use of benzofuran-7-carboxamide as the aroyl moiety led to a substantial increase of 5HT3 receptor affinity.The optimal 5HT3 receptor antagonist identified via extensive SAR studies was endo-5-chloro-2,3-dihydro-2,2-dimethyl-N-(8-methyl-8-azabicyclooct-3-yl)-7-benzofurancarboxamide (Z)-2-butenedioate (zatosetron maleate).The 7-carbamyl regiochemistry, dimethyl substitution, chloro substituent, and endo stereochemistry were all crucial elements of the SAR.Zatosetron maleate was a potent antagonist of 5HT-induced bradycardia in rats (ED50=0.86 μg/kg iv).Low oral doses of zatosetron (30 μg/kg) produced long-lasting antagonism of 5HT3 receptors, as evidenced by blockade of 5HT-induced bradycardia for longer than 6 h in rats.Moreover, this compound did not produce hemodynamic effects after iv administration to rats, nor did it block carbamylcholine-induced bradycardia in doses that markedly blocked 5HT3 receptors.Thus, zatosetron is a potent, selective, orally effective 5HT3 receptor antagonist with a long duration of action in rats.
- Robertson, David W.,Lacefield, William B.,Bloomquist, William,Pfeifer, William,Simon, Richard L.,Cohen, Marlene L.
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p. 310 - 319
(2007/10/02)
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- Benzothiophenes and benzofurans and antiallergic use thereof
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Novel benzothiophene and benzofuran derivatives having antiallergic activity are described as well as a method of manufacture, pharmaceutical compositions, and methods of use therefor. The disclosure describes the use of derivatives for prevention of the release of mediators including histamine and leukotrienes from basophils and mast cells, and prevent respiratory burst in neutrophils providing activity useful in cardiovascular disorders as well as in antiinflammatory, psoriasis, and antimigraine treatment.
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- Antibacterial benzo(chalcogeno)[4,3,2-cd]indazoles
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Substituted 2H-[1]benzopyrano[4,3,2-cd]indazoles, 2H-[1]benzothiopyrano[4,3,2-cd]indazoles, and 2H-[1]benzoselenino[4,3,2-cd]indazoles have demonstrated pharmacological activity against a broad spectrum of Gram-positive and Gram-negative bacteria, yeasts,
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- A New Regiospecific Synthesis of 1,4-Dihydroxyxanthones
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Several methyl salicylates have been found to substitute halogenated benzoquinones regiospecifically in the presence of anhydrous potassium fluoride.The resultant phenoxybenzoquinones were reduced and cyclized to highly functionalized xanthones of unambig
- Simoneau, Bruno,Brassard, Paul
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p. 1507 - 1510
(2007/10/02)
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