- Properties of plasmodium falciparum with a deleted apicoplast DNA gyrase
-
Malaria parasites have three genomes: a nuclear genome, a mitochondrial genome, and an apicoplast genome. Since the apicoplast is a plastid organelle of prokaryotic origin and has no counterpart in the human host, it can be a source of novel targets for a
- Kokkonda, Sreekanth,Mudeppa, Devaraja G.,Patrapuvich, Rapatbhorn,Rathod, Pradipsinh K.,Tan, Soo Nee,White, John
-
supporting information
(2021/08/23)
-
- Palladium-Catalyzed Carbamoyl-Carbamoylation/ Carboxylation/Thioesterification of Alkene-Tethered Carbamoyl Chlorides Using Mo(CO)6 as the Carbonyl Source
-
We reported a palladium-catalyzed carbamoyl-carbamoylation/carboxylation/thioesterification of alkene-tethered carbamoyl chlorides using Mo(CO)6 as the carbonyl source. The reactions were typically performed with good functional group compatibility and tolerated different nucleophiles (amines, alcohols, phenols, thiols and water), which provided a new access to amidated/esterificated/thioesterificated/carboxylated oxindoles or lactams bearing an all-carbon quaternary stereocenter under CO gas-free conditions. Furthermore, natural product mutation and divergent late-stage derivatization are the important practical features.
- Chen, Chen,Ding, Jie,Huang, Yujie,Liu, Liying,Zhu, Bolin
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supporting information
(2022/01/04)
-
- Ruthenium Metathesis: A Key Step to Access a New Cyclic Tetrasubstituted Olefin Platform
-
An rapid and mild synthetic route for the preparation of cyclic tetrasubstituted platforms via ruthenium-catalyzed ring-closing metathesis (RCM) has been developed. This process tolerates a wide range of functionalities such as nitrogen, oxygen, sulfur, silicon, and carbon tethered groups, as well as very challenging fluorine and boron atoms (36 derivatives, up to 96%). This diversity-oriented method was further demonstrated by the postfunctionalization reactions, such as Pd-couplings, N-substitution, and reductive amination introducing a morpholine moiety.
- Heinrich, Clément F.,Durand, Didier,Starck, Jér?me,Michelet, Véronique
-
supporting information
p. 7064 - 7067
(2020/08/24)
-
- Pd-catalyzed regiodivergent synthesis of diverse oxindoles enabled by the versatile heck reaction of carbamoyl chlorides
-
We report herein a miscellaneous oxindole synthesis bearing an all-carbon quaternary center, enabled by Pd-catalyzed intramolecular cyclization followed by multiple intermolecular Heck reactions of both easily accessible alkene-tethered carbamoyl chlorides and olefins. This protocol obviates the use of prefunctionalized olefinic reagents, exhibits excellent functional group tolerance, and features fascinating reactive versatility.
- Wu, Xianqing,Tang, Zaiquan,Zhang, Chengxi,Wang, Chenchen,Wu, Licheng,Qu, Jingping,Chen, Yifeng
-
supporting information
p. 3915 - 3921
(2020/06/08)
-
- Enantioselective Construction of Tertiary Fluoride Stereocenters by Organocatalytic Fluorocyclization
-
1,1-Disubstituted styrenes with internal oxygen and nitrogen nucleophiles undergo oxidative fluorocyclization reactions with in situ generated chiral iodine(III)-catalysts. The resulting fluorinated tetrahydrofurans and pyrrolidines contain a tertiary carbon-fluorine stereocenter. Application of a new 1-naphthyllactic acid-based iodine(III)-catalyst allows the control of tertiary carbon-fluorine stereocenters with up to 96% ee. Density functional theory calculations are performed to investigate the details of the mechanism and the factors governing the stereoselectivity of the reaction.
- Biosca, Maria,Eriksson, Lars,Hedberg, Martin,Himo, Fahmi,Lübcke, Marvin,Szabó, Kálmán J.,Wang, Qiang
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supporting information
p. 20048 - 20057
(2020/11/27)
-
- Aminoxyl-Catalyzed Electrochemical Diazidation of Alkenes Mediated by a Metastable Charge-Transfer Complex
-
We report the development of a new aminoxyl radical catalyst, CHAMPO, for the electrochemical diazidation of alkenes. Mediated by an anodically generated charge-transfer complex in the form of CHAMPO-N3, radical diazidation was achieved across a broad scope of alkenes without the need for a transition metal catalyst or a chemical oxidant. Mechanistic data support a dual catalytic role for the aminoxyl serving as both a single-electron oxidant and a radical group transfer agent.
- Siu, Juno C.,Parry, Joseph B.,Lin, Song
-
supporting information
p. 2825 - 2831
(2019/02/14)
-
- Ligand-Promoted Iron(III)-Catalyzed Hydrofluorination of Alkenes
-
An iron-catalyzed hydrofluorination of unactivated alkenes has been developed. The use of a multidentate ligand and the fluorination reagent N-fluorobenzenesulfonimide (NFSI) proved to be critical for this reaction, which afforded various fluorinated comp
- Xie, Yongtao,Sun, Peng-Wei,Li, Yuxin,Wang, Siwei,Ye, Mengchun,Li, Zhengming
-
p. 7097 - 7101
(2019/04/17)
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- Direct Hydrofluorination of Methallyl Alkenes Using a Methanesulfonic Acid/Triethylamine Trihydrofluoride Combination
-
The use of a methanesulfonic acid/triethylamine trihydrofluoride combination for the direct hydrofluorination of methallyl-containing substrates is reported. Under those metal-free conditions that use readily available, cheap, and easy to handle reagents,
- Bertrand, Xavier,Paquin, Jean-Fran?ois
-
supporting information
p. 9759 - 9762
(2019/11/28)
-
- BENZIMIDAZOLONE DERIVED INHIBITORS OF BCL6
-
The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity: wherein X1, X2, R1, R2 and R3 are each as defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which BCL6 activity is implicated.
- -
-
Paragraph 00373; 00375
(2018/12/13)
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- Hydropyridylation of Olefins by Intramolecular Minisci Reaction
-
An unprecedented cheap, mild and easy methodology for an intramolecular Minisci reaction based on a hydrogen atom transfer (HAT) initiated hydrofunctionalization of olefins was developed. The method is suitable for the construction of unusual dihydropyrano-pyridine and 1,2,3,4-tetrahydronaphthiridine structures and, unlike most similar reactions, does not require exclusion of air from the reaction medium.
- Bordi, Samuele,Starr, Jeremy T.
-
supporting information
p. 2290 - 2293
(2017/05/12)
-
- Real-Time Biological Annotation of Synthetic Compounds
-
Organic chemists are able to synthesize molecules in greater number and chemical complexity than ever before. Yet, a majority of these compounds go untested in biological systems, and those that do are often tested long after the chemist can incorporate t
- Gerry, Christopher J.,Hua, Bruce K.,Wawer, Mathias J.,Knowles, Jonathan P.,Nelson, Shawn D.,Verho, Oscar,Dandapani, Sivaraman,Wagner, Bridget K.,Clemons, Paul A.,Booker-Milburn, Kevin I.,Boskovic, Zarko V.,Schreiber, Stuart L.
-
supporting information
p. 8920 - 8927
(2016/07/30)
-
- Expedient Access to 2,3-Dihydropyridines from Unsaturated Oximes by Rh(III)-Catalyzed C-H Activation
-
α,β-Unsaturated oxime pivalates are proposed to undergo reversible C(sp2)-H insertion with cationic Rh(III) complexes to furnish five-membered metallacycles. In the presence of 1,1-disubstituted olefins, these species participate in irreversible migratory insertion to give, after reductive elimination, 2,3-dihydropyridine products in good yields. Catalytic hydrogenation can then be used to convert these molecules into piperidines, which are important structural components of numerous pharmaceuticals.
- Romanov-Michailidis, Fedor,Sedillo, Kassandra F.,Neely, Jamie M.,Rovis, Tomislav
-
supporting information
p. 8892 - 8895
(2015/08/03)
-
- The compound having a polymerizable liquid crystal oxyranyl groups, and polymer compsn.
-
The main aim of the invention is to provide a polymerizable liquid crystal compound that has a liquid crystal phase with a wide temperature range centering at room temperature, has an excellent compatibility with another polymerizable liquid crystal compo
- -
-
Paragraph 0149
(2019/06/27)
-
- Synthesis of substituted cycloalkene-1,1-dicarboxylates via olefin metathesis in water
-
A range of substituted cycloalkene-1,1-dicarboxylates was synthesized through olefin metathesis starting from readily available acylic malonate precursors in an efficient fashion. As a metathesis catalyst, a Grubbs II-type catalyst was used in these exper
- Tenbrink, Katharina,Kemker, Isabell,Schatz, Jürgen,Gr?ger, Harald
-
-
- Synthesis of 3-fluoropyrrolidines and 3-fluoroazetidines
-
A synthetic route towards 1-t-butoxycarbonyl-3-fluoro-3-methylpyrrolidine and 1-tbutoxycarbonyl 3-fluoro-3-methylazetidine, which are interesting building blocks for pharmaceutical compounds, is described. The key steps include a bromofluorination of appr
- Piron, Karel,Verniest, Guido,Van Hende, Eva,De Kimpe, Norbert
-
scheme or table
p. 6 - 15
(2012/03/10)
-
- Cu(II)-Catalyzed Olefin Migration and Prins Cyclization: Highly Diastereoselective Synthesis of Substituted Tetrahydropyrans
-
Metal-ligand complexes of Cu(OTf)2 with an appropriate bisphosphine ligand have been shown to effectively catalyze the formation of substituted tetrahydropyrans via a sequential olefin migration and Prins-type cyclization. This methodology provides convenient access to a variety of functionalized tetrahydropyrans in excellent diastereoselectivities and good to excellent yields.
- Ghosh, Arun K.,Nicponski, Daniel R.
-
supporting information; experimental part
p. 4328 - 4331
(2011/10/05)
-
- Aminocyclopropanes as precursors of endoperoxides with antimalarial activity
-
This contribution describes the synthesis of several novel bicyclic α-amino endoperoxides, including CF3-substituted compounds, prepared by the aerobic electrochemical oxidation of a family of bicyclic aminocyclopropanes. These, in turn, are re
- Madelaine, Claire,Buriez, Olivier,Crousse, Benoit,Florent, Isabelle,Grellier, Philippe,Retailleau, Pascal,Six, Yvan
-
supporting information; experimental part
p. 5591 - 5601
(2011/02/18)
-
- A detailed investigation of the aza-prins reaction
-
The development of a Lewis acid-promoted aza-Prins reaction to form piperidines and pyrrolidines is described. Indium trichloride has been found to be a highly successful and mild Lewis acid for promoting this reaction. A thorough mechanistic investigation is described, including the factors that influence the formation of the 5- or 6-membered ring product(s). The Royal Society of Chemistry.
- Dobbs, Adrian P.,Guesne, Sebastien J. J.,Parker, Robert J.,Skidmore, John,Stephenson, Richard A.,Hursthouse, Mike B.
-
supporting information; experimental part
p. 1064 - 1080
(2010/06/13)
-
- NEW CLASS OF GAMMA DELTA T CELLS ACTIVATORS AND USE THEREOF
-
The present invention relates to a new class of compounds having γδ T cells activating properties, a composition comprising these compounds and methods for regulating an immune response in a subject comprising the step of administering these compounds.
- -
-
Page/Page column 39
(2008/06/13)
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- COMPOSITION AND METHOD FOR THE TREATMENT OF CARCINOMA
-
The present invention relates to compositions and methods useful for treating a carcinoma or viral infection in mammals, including humans. The methods and compositions typically comprise use of an immunogenic or immunomodulatory compound, and a γδT cell a
- -
-
Page/Page column 74
(2008/06/13)
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- Stereochemical analysis of isopentenyl diphosphate isomerase type II from Staphylococcus aureus using chemically synthesized (S)- and (R)-[2- 2H]Isopentenyl diphosphates
-
(Chemical Equation Presented) To study the catalysis of isopentenyl diphosphate (IPP) isomerase type II from Staphylococcus aureus, which is a flavoprotein catalyzing the interconversion of IPP and dimethylallyl diphosphate, we have chemically synthesized (S)- and (R)-[2-2H]IPP and carried out stereochemical analysis of the reaction. Our results show that the C-2 deprotonation of IPP by this enzyme is pro-R stereospecific, suggesting a similar stereochemical course as the type I enzyme.
- Kao, Chai-Lin,Kittleman, William,Zhang, Hua,Seto, Haruo,Liu, Hung-Wen
-
p. 5677 - 5680
(2007/10/03)
-
- Phosphalohydrins and methods for medicinal administration
-
The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3and —CH2—CH3, Cat+ is an organic or inorgan
- -
-
Page column 15-16
(2008/06/13)
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- Catalytic and stoichiometric Lewis acid participation in aldehyde ene cyclisations
-
Racemic 2-isopropyl-2-methylhex-5-enal has been synthesised in order to probe ene cyclisations leading to menthol analogues. The objective was first to discover catalytic conditions for preferential cyclisation to the menthol rather than the neomenthol series and then to develop (dynamic) kinetic resolution procedures which afforded a single enantiomer of product. It was found that catalytic quantities of both Me2AlCl and a bulky methyl-aluminium bis(phenoxide) reagent gave products attributed to a Meerwein-Pondorff-Verley reaction. In this the aldehyde is reduced to a primary alcohol and the ene product oxidised to the corresponding α,β-unsaturated ketone. By contrast, a related bulky chloroaluminium reagent catalysed the ene cyclisation cleanly, but preferentially to the undesired neomenthyl stereoisomer.
- Braddock, D. Christopher,Brown, John M.
-
p. 741 - 756
(2007/10/03)
-
- Peroxycarbenium-mediated C-C bond formation: Applications to the synthesis of hydroperoxides and peroxides
-
The Lewis acid-mediated reaction of alkene nucleophiles with peroxyacetals provides an effective route for the synthesis of homologated peroxides and hydroperoxides. In the presence of Lewis acids such as TiCl4, SnCl4, and trimethylsilyl triflate, peroxyacetals and peroxyketals undergo reaction with allyltrimethylsilane, silyl enol ethers, and silyl ketene acetals to afford homoallyl peroxides, 3-peroxyketones, and 3-peroxyalkanoates, respectively. Reactions of peroxyacetals are Lewis acid dependent; TiCl4 promotes formation of ethers while SnCl4 and trimethylsilyl triflate promote formation of peroxides. Lewis acid-promoted reactions of silylated hydroperoxyacetals furnish silylated hydroperoxides, which can be deprotected to homologated hydroperoxides. Hydroperoxyketals undergo Lewis acid-mediated allylation to furnish 1,2-dioxolanes via attack of hydroperoxide on the intermediate carbocation. Lewis acid-mediated cyclization of unsaturated peroxyacetals furnishes 1,2-dioxanes, 1,2-dioxepanes, and 1,2-dioxacanes through 6-endo/exo, 7-endo/endo, and 8-endo/endo pathways. The corresponding reactions involving 6-endo/endo and 5-endo/exo pathways were unsuccessful.
- Dussault,Lee, In Quen,Lee,Lee,Niu,Schultz,Zope
-
p. 8407 - 8414
(2007/10/03)
-
- Ring-closing metathesis of titanium - Carbene complexes prepared from thioacetals having a carbon - Carbon double bond
-
The ring-closing metathesis proceeded to give cycloalkenes in good yields when diphenyl thioacetals having a carbon-carbon double bond were treated with the low-valent titanium species Cp2Ti[P(OEt)3]2 in THF at room temperature and then at reflux. This methodology is successfully applied to the preparation of cyclic ethers and sulfides. (C) 2000 Published by Elsevier Science Ltd.
- Fujiwara, Tooru,Kato, Yoshiko,Takeda, Takeshi
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p. 4859 - 4869
(2007/10/03)
-
- Transformation of presumptive precursors to frontalin and ex-brevicomin by bark beetles and the West Indian sugarcane weevil (Coleoptera)
-
(Z)-6-Nonen-2-one (1) has recently been shown to be the biosynthetic precursor for the aggregation pheromone exo-brevicomin (2) in mountain pine beetle (MPB) males, Dendroctonus ponderosae (Hopkins). We tested the hypotheses that (1) 6-methyl-6-hepten-2-one (3) is the biosynthetic precursor for the aggregation pheromone frontalin (4) in the spruce beetle (SB), Dendroctonus rufipennis (Kirby), and (2) that frontalin and exo-brevicomin are produced from 3 and 1, respectively, only by beetles that utilize them as aggregation pheromones. Exposure of scolytids MPB, SB, pine engraver (PE), Ips pini (Say) and Ips tridens (Mannerheim) and West Indian sugar cane weevil (WISW), Metamasius hemipterus sericeus (Olivier) to deuterio- or protio-3 invariably resulted in the production of deuterio- or protio-4. Similarly, exposure of SB, WISW and I. tridens to 1 resulted in the production of 2. We were unable to demonstrate the presence of 3 in SB volatiles, nor were we able to demonstrate the conversion of 6-methyl-5-hepten-2-one to 3 by SB. Production of enantiomerically enriched frontalin and exo-brevicomin by all the beetles exposed to respective precursors reveals widespread occurrence of nonspecific polysubstrate monooxidases in the Coleoptera.
- Perez,Gries,Gries,Oehlschlager
-
p. 445 - 450
(2007/10/03)
-
- Synthesis of pyrrolidines and piperidines via palladium-catalyzed coupling of vinylic halides and olefinic sulfonamides
-
The palladium-catalyzed coupling of vinylic halides and olefinic sulfonamides affords good yields of 2-(1-alkenyl)pyrrolidine and -piperidine sulfonamides via vinylpalladium addition to the olefin, regioselective rearrangement to a π-allylpalladium intermediate, and subsequent intramolecular nucleophilic displacement of palladium.
- Larock,Yang,Weinreb,Herr
-
p. 4172 - 4178
(2007/10/02)
-
- Enantioselective intramolecular cyclopropanation of N-allylic-and N-homoallylic diazoacetamides catalyzed by chiral dirhodium(II) catalysts
-
Diazodecomposition of N-(tert-butyl)-N-(3-buten-1-yl)diazoacetamides catalyzed by dirhodium(II) tetrakis[methyl 2-pyrrolidone-5(S)-carboxylate], Rh2(5S-MEPY)4, and tetrakis[methyl 2-oxazolidinone-4(S)-carboxylate], Rh2(4S-
- Doyle, Michael P.,Eismont, Michail Y.,Protopopova, Marina N.,Kwan, Michelle M. Y.
-
p. 1665 - 1674
(2007/10/02)
-
- Cyclization of farnesyl diphosphate to pentalenene. Orthogonal stereochemistry in an enzyme-catalyzed S(E') reaction
-
Pentalenene synthase catalyzes the cyclization of farnesyl diphosphate to (1) the sesquiterpene hydrocarbon pentalenene (4). Separate incubations of (4S,8S)-[4,8-3H2, 4,8-14C2]farnesyl diphosphate and (4R,8R)-[4,8-3H2, 4,814C2]farnesyl diphosphate with pentalenene synthase isolated from Streptomyces UC5319 and analysis of the derived labeled pentalenenes, 4a and 4b, respectively, by chemical degradation established that H-8si of FPP was lost upon cyclization to pentalenene. Consideration of the plausible conformations of the enzymatic cyclization intermediates indicates that the electrophilic allylic addition elimination (S(E')) reaction in which the C-4,5 bond of pentalenene is formed involves an orthogonal relationship between the C-C bond being formed and the C-H bond that is ultimately broken.
- Cane,Weiner
-
p. 118 - 127
(2007/10/02)
-
- Asymmetric Synthesis of Pipecolic Acid Derivatives
-
Condensation of chiral N-homoallyl β-amino alcohols with glyoxal produces iminium ions which are cyclized with complete stereoselectivity.These substrates, whose reactivity is closely dependent on the substitution pattern of the ethylenic moiety, undergo
- Agami, Claude,Couty, Francois,Poursoulis, Michel,Vaissermann, Jacqueline
-
p. 431 - 442
(2007/10/02)
-
- Homolytic Displacement at Saturated Carbon: Part 5. Synthesis of Cyclopropylmethyl, Bicyclohex-2-yl, Bicyclohept-2-yl and Cyclohexanespirocycloprop-2-yl Sulphones from the Corresponding But-3-enylcobaloximes
-
But-3-enylcobaloxime reacts with arenesulphonyl chlorides under thermal and photochemical conditions to give cyclopropylmethyl sulphones.The yields depend upon the reaction conditions used.Similar reactions of cyclopent-2-enylmethylcobaloxime and cyclohex-2-enylmethylcobaloximes under photochemical conditions form a mixture of cis and trans isomers of bicyclohex-2-yl and bicyclohept-2-yl sulphones in (50:50) and (70:30) isomeric ratios respectively.However, cyclohex-3-enylcobaloximes form only the trans-bicyclohex-2-yl sulphone.Exclusive formation of cycloalkanespirocycloprop-2-yl sulphones is observed in the reactions of 2-(cyclo alk-1-enyl)ethylcobaloximes with arenesulphonyl chlorides.The reactions are free radical in nature and are believed to take place by a chain mechanism.In the key step a homolytic attack of the RSO2 radical at the terminal (δ) carbon of the butenyl ligand leads to the cyclized product.The exact nature of the ring closure step is uncertain, as both concerted and stepwise mechanisms are possible.
- Gupta, B. Dass,Das, Indira,Dixit, Vandana
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p. 2409 - 2446
(2007/10/02)
-
- STEREOSELECTIVE REDUCTION OF ACETALS. A METHOD FOR REDUCTIVE GENERATION OF HETEROCYCLIC RING SYSTEMS
-
A new synthetic process for the construction of oxygen-containing heterocyclic systems starting from bicyclic acetals is described.We have investigated the mechanism and the stereochemical course of the reductive cleavage of acetals.
- Ishihara, Kazuaki,Mori, Atsunori,Yamamoto, Hisashi
-
p. 4595 - 4612
(2007/10/02)
-
- SYNTHESIS OF α-NERYL AND α-GERANYL PROPIONATES - COMPONENTS OF THE SEX PHEROMONE OF SAN JOSE SCALE
-
α-Neryl and α-geranyl propionates - components of the sex pheromone of San Jose scale - have been synthesized by the two-stage E/ Z-C5 homologization of isopentenyl iodide.
- Moiseenkov, A. M.,Ishchenko, R. I.,Veselovskii, V. V.,Odinokov, V. N.,Polunin, E. V.,et al.
-
p. 366 - 368
(2007/10/02)
-
- PREPARATIVE SYNTHESIS OF TOSYLATES OF UNSATURATED ALCOHOLS AND UNSATURATED BROMIDES UNDER PHASE TRANSFER CONDITIONS
-
A preparative synthetic method has been developed for tosylates of unsaturated alcohols and their conversion to bromides under phase transfer conditions in the case of alkyn-1-ols, E- and Z-alken-1-ols, 3-methyl-3-buten-1-ol and cyclopropylmethanol.
- Ishchenko, R. I..,Kovalev, B. G.,Khusid, A. Kh.
-
p. 1076 - 1078
(2007/10/02)
-
- PHOTOENOLISATION OF CONJUGATED ESTERS: SYNTHESIS OF A SAN JOSE SCALE PHEROMONE BY PARTIALLY REGIO-CONTROLLED PHOTOCHEMICAL DECONJUGATION.
-
The photochemical deconjugation reaction of an α,β-unsaturated ester is applied to the synthesis of one of the components of the San Jose scale pheromone, compound 1.The use of a weak organic base as a means of control of the regiochemistry of the deconjugation reaction was demonstrated.
- Lombardo, Domenic A.,Weedon, Alan C.
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p. 5555 - 5558
(2007/10/02)
-
- Phosphorylation of Isoprenoid Alcohols
-
Procedures for the synthesis and purification of 20 isoprenoid diphosphates and methanediphosphonate analogues from the corresponding alcohols are described.The alcohols are activated for phosphorylation by conversion of homoallylic systems to tosylates and allylic systems to halides.The activated intermediates are treated with tris(tetra-n-butylammonium) salts of pyrophosphoric, methanediphosphonic, or difluoromethanediphosphonic acid to obtain the corresponding esters in yields 34-80percent.Chromatography on cellulose is a general method for purification of isoprenoid diphosphates, and procedures are decribed for compounds with C5 to C20 hydrocarbon moieties.The displacement by pyrophosphate occurs with inversion of configuration, and the procedure can be used to prepare isoprenoid diphosphates with chiral C1 methylene groups in high optical purity from the corresponding alcohols.
- Davisson, V. Jo,Woodside, Andrew B.,Neal, Timothy R.,Stremler, Kay E.,Muehlbacher, Manfred,Poulter, C. Dale
-
p. 4768 - 4779
(2007/10/02)
-
- Lewis-acid Promoted Aromatic Cyclization of &α-Chlorosulfides: Synthesis of Ethyl Isothiochroman-1-carboxylate and Related Compounds
-
A variety of ethyl isothiochroman-1-carboxylates and related compounds were synthesized by treatment of 2-chloro-2-acetates with stannic chloride in methylene chloride.The same procedure was applied to the synthesis of ethyl 4-chloro-4-methyltetrahydrothiopyran-2-carboxylate.Some isothiochroman-1-carboxylic acids were prepared and evaluated for antiinflammatory activity.Among the compounds tested, 7-phenoxyisothiochroman-1-carboxylic acid showed weak activity.
- Ishibashi, Hiroyuki,Okada, Motofumi,Iida, Kyoko,Ikeda, Masazumi
-
p. 1527 - 1529
(2007/10/02)
-
- O-SILYLATED ENOLATE PHENYLTHIOALKYLATION: A NEW SYNTHESIS OF UNSATURATED 1,5-DICARBONYL COMPOUNDS.
-
The O-silylated enolates of ketones and esters can be phenylthioalkylated by the chlorides (2) and (3) under ZnBr2-catalysis; ozonolysis and subsequent sulphoxide thermolysis then gives the corresponding unsaturated 1,5-dicarbonyl compounds.
- Khan, Hassan A.,Paterson, Ian
-
p. 2399 - 2402
(2007/10/02)
-
- 1,3-DIYL TRAPPING REACTIONS. FUNDAMENTAL INVESTIGATIONS WITH APPLICATION TO THE SYNTHESIS OF LINEARLY FUSED TRICYCLOPENTANOIDS
-
A comparison of the inter- and intramolecular diyl trapping routes to linearly fused tricyclopentanoids is presented.In addition, several of the factors which are responsible for the stereoselectivity which is associated with the intramolecular process ar
- Little, R. Daniel,Muller, George W.,Venegas, Manuel G.,Caroll, Gary L.,Bukhari, Ahmed,et al.
-
p. 4371 - 4384
(2007/10/02)
-
- 1,3-diyl trapping reactions. Fundamental investigations with application to the synthesis of linearly fused tricyclopentanoids
-
A comparison of the inter- and intramolecular diyl trapping routes to linearly fused tricyclopentanoids is presented. In addition, several of the factors which are responsible for the stereoselectivity which is associated with the intramolecular process a
- Little, R. Daniel,Muller, George W.,Venegas, Manuel G.,Carroll, Gary L.,Bukhari, Ahmed,Patton, Larry,Stone, Keith
-
p. 4371 - 4383
(2014/12/11)
-