- Direct synthesis of G-2N
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The synthesis of angularly fused quinone natural products has been achieved using a photoenolization reaction and a Diels-Alder reaction in the key carbon-carbon bond forming steps.
- Kraus, George A.,Zhao, Guohua
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Read Online
- A Pyrolytic Approach to 2-Hydroxy-7-methoxy-5-methyl-1-naphthoic Acid
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Condensation of 4-methoxy-2,6-dimethylbenzaldehyde with Meldrum's acid, and flash vacuum pyrolysis of the condensation product (12) gave in almost quantitative yield 7-methoxy-5-methyl-2-naphthol (9).This naphthol is a precursor of the title 1-carboxylic acid (6), an intercalating moiety of enediyne and other antibiotics.
- Brown, Roger F. C.,Eastwood, Frank W.,Horvath, Julianna
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Read Online
- Formylation of electron-rich aromatic rings mediated by dichloromethyl methyl ether and TiCl4: Scope and limitations
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Here the aromatic formylation mediated by TiCl4 and dichloromethyl methyl ether previously described by our group has been explored for a wide range of aromatic rings, including phenols, methoxy- and methylbenzenes, as an excellent way to produce aromatic aldehydes. Here we determine that the regioselectivity of this process is highly promoted by the coordination between the atoms present in the aromatic moiety and those in the metal core.
- Ramos-Tomillero, Iván,Paradís-Bas, Marta,De Pinho Ribeiro Moreira, Ibério,Bofill, Josep María,Nicolás, Ernesto,Albericio, Fernando
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supporting information
p. 5409 - 5422
(2015/05/13)
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- A direct and mild formylation method for substituted benzenes utilizing dichloromethyl methyl ether-silver trifluoromethanesulfonate
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A silver trifluoromethanesulfonate (AgOTf)-promoted direct and mild formylation of benzenes has been developed. The reaction utilizing dichloromethyl methyl ether (Cl2CHOMe) and AgOTf powerfully formylated various substituted benzenes under temperature conditions as low as -78 C without losing the protecting groups on the phenolic hydroxyl group.
- Ohsawa, Kosuke,Yoshida, Masahito,Doi, Takayuki
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p. 3438 - 3444
(2013/06/26)
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- Acid-labile cys-protecting groups for the Fmoc/tBu strategy: Filling the gap
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To address the existing gap in the current set of acid-labile Cys-protecting groups for the Fmoc/tBu strategy, diverse Fmoc-Cys(PG)-OH derivatives were prepared and incorporated into a model tripeptide to study their stability against TFA. S-Dpm proved to be compatible with the commonly used S-Trt group and was applied for the regioselecive construction of disulfide bonds.
- Gongora-Benitez, Miriam,Mendive-Tapia, Lorena,Ramos-Tomillero, Ivan,Breman, Arjen C.,Tulla-Puche, Judit,Albericio, Fernando
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supporting information
p. 5472 - 5475,4
(2012/12/12)
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- Acid-labile cys-protecting groups for the Fmoc/tBu strategy: Filling the gap
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To address the existing gap in the current set of acid-labile Cys-protecting groups for the Fmoc/tBu strategy, diverse Fmoc-Cys(PG)-OH derivatives were prepared and incorporated into a model tripeptide to study their stability against TFA. S-Dpm proved to be compatible with the commonly used S-Trt group and was applied for the regioselecive construction of disulfide bonds.
- Góngora-Benítez, Miriam,Mendive-Tapia, Lorena,Ramos-Tomillero, Iván,Breman, Arjen C.,Tulla-Puche, Judit,Albericio, Fernando
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supporting information
p. 5472 - 5475
(2013/01/15)
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- Synthesis of novel structurally simplified estrogen analogues with electron-donating groups in ring A
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A library of 25 novel estrogen analogues were prepared in five to eight steps from mostly commercially available substituted anisoles via bromination, formylation, Corey-Fuchs reaction, elimination, and Sonogashira reaction. Georg Thieme Verlag Stuttgart.
- Tietze, Lutz F.,Vock, Carsten A.,Krimmelbein, Ilga K.,Nacke, Linda
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experimental part
p. 2040 - 2060
(2009/12/27)
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- THYROID HORMONE ANALOGUES AND METHODS FOR THEIR PREPARATION
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Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.
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Page/Page column 21
(2010/02/11)
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- De novo design, synthesis, and evaluation of novel nonsteroidal phenanthrene ligands for the estrogen receptor
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Although there are many estrogen receptor antagonists with improved tissue selectivity profiles compared with tamoxifen, optimal tissue selectivity has not yet been demonstrated. As such there is still a need for additional diversity and new chemical scaf
- Schmidt, Jonathan M.,Mercure, Julie,Tremblay, Gilles B.,Pagé, Martine,Kalbakji, Aida,Feher, Miklos,Dunn-Dufault, Robert,Peter, Markus G.,Redden, Peter R.
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p. 1408 - 1418
(2007/10/03)
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- Non-steroidal estrogen receptor ligands
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Novel non-steroidal estrogen receptor ligands and methods of synthesis are disclosed. The novel molecules are intended for use in therapeutic preparations for the treatment of estrogen receptor related disease states. The compounds specified are tetra-cyc
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- An enantiospecific approach to 8,9-seco-C-aromatic taxanes
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An enantiospecific approach to functionalised C-aromatic-8,9-seco-taxanes starting from the readily available monoterpene (R)-carvone is described.
- Srikrishna,Ravi Kumar,Padmavathi
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p. 1907 - 1909
(2007/10/03)
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- Thyroid hormone analogues and methods for their preparation
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Thyroid hormone analogues are disclosed. Methods of using such analogues and pharmaceutical compositions containing them are also disclosed, as are novel procedures for their preparation.
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- Selective thyroid hormone analogs
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Selective thyroid hormone agonists are disclosed that are highly selective for the TR beta subtype with high binding affinity. Methods of using such agonists and pharmaceutical compositions containing them are also disclosed, as are novel procedures for
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- Ring-chain tautomerism, oxidation, and NO-reaction of a sterically hindered 1,3-dihydroxyimidazolidine
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The bis-hydroxylamine 1 does not react with the hindered benzaldehyde 2 in ethanolic solution, in DMSO or DMF even at high temperatures. Reaction only takes place after melting the components without any solvent at about 150°C. The product shows ring-chai
- Weber,Grzesiok
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p. 823 - 827
(2007/10/03)
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- Stereoselective total synthesis of topographically constrained designer amino acids: 2',6'-dimethyl-β-methyltyrosines
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The constrained aromatic α-amino acid 2',6'-dimethyl-β-methyl tyrosine (Figure 1) was designed to provide specific local constraints to peptides or peptide mimetics. We report here methods for the total asymmetric synthesis of all four stereoisomers. The
- Qian,Russell,Boteju,Hruby
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p. 1033 - 1054
(2007/10/02)
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- Process for formylation of aromatic compounds
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A process for the preparation of a formylated aromatic compound comprising contacting an aromatic compound with (i) a halogenated compound in the presence of a Lewis acid, and (ii) a base, is described. The subject process provides an efficient and effect
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- Ring-Substituted y1,2-Bis(4-hydroxyphenyl)ethylenediamine>dichloroplatinum(II) Complexes: Compounds with a Selective Effect on the Hormone-Dependent Mammary Carcinoma
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dichloroplatinum(II) complexes with one substituent in the 2-position (CH3, CF3, F, Br, I: meso- and dl-1-PtCl2, meso-(3-5)-PtCl2, meso-(7 and 8)-PtCl2) or two substituents in the 2,6-position (CH3, Cl: meso-2-PtCl2, meso- and dl-6-PtCl2) in both benzene rings were synthesized and tested for estrogenic and toxic activities.Two complexes (meso-6-PtCl2 and meso-7-PtCl2) possess both effects.In comparative tests on estrogen receptor positive and negative mammary tumors in cell culture (MCF 7, ER+ and MDA-MB 231, ER-) and in animals (MXT, ER+ and MXT, ER-, mouse), meso-6-PtCl2 shows a selective effect on the estrogen receptor positive mammary carcinoma.A further increase of efficacy was achieved with the water-soluble (sulfato)platinum(II) derivative (meso-6-PtSO4).On the DMBA-induced hormone dependent mammary carcinoma of the SD rat, meso-6-PtSO4 is significantly more active than its ligand (meso-6) and cisplatin.
- Karl, Johann,Gust, Ronald,Spruss, Thilo,Schneider, Martin R.,Schoenenberg, Helmut,et al.
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- Potential antisecretory antidiarrheals. 1. α2-Adrenergic aromatic aminoguanidine hydrazones
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Guanabenz, a centrally acting antihypertensive agent, has been shown to have intestinal antisecretory properties. A series of aromatic aminoguanidine hydrazones was made in an effort to separate the antisecretory and cardiovascular activities. Benzaldehyde, naphthaldehyde, and tetralone derivatives were synthesized. The compounds were evaluated in the cholera toxin treated ligated jejunum of the rat and in the Ussing chamber using a rabbit ileum preparation. A number of compounds, including members of each structural class, were active upon subcutaneous administration in the rat. Active compounds were determined to be α2-adrenergic agonists by yohimbine reversals of their Ussing chamber activities. The compound displaying the best separation of activities was the aminoguanidine hydrazone of 2,6-dimethyl-4-hydroxybenzaldehyde (20).
- Pitzele,Moormann,Gullikson,Albin,Bianchi,Palicharla,Sanguinetti,Walters
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p. 138 - 144
(2007/10/02)
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- Syntheses of 4-Hydroxy-2,6-dimethylbenzoic Acid and Its Higher Homologues
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Syntheses of 4-hydroxy-2,6-dimethylbenzoic acid (2a) and its higher homologues, viz 4-hydroxy-2,6-dimethylphenylacetic acid (2b), 3-(4-hydroxy-2,6-dimethylphenyl)propanoic acid (2c) and 4-(4-hydroxy-2,6-dimethylphenyl)butanoic acid (2d) are described.
- Bhattacharya, Kalyan K.,Pal, Panchanan,Ghosh, Kalpana,Sen, P. K.
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p. 191 - 194
(2007/10/02)
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