- CYCLOALKYL-CONTAINING CARBOXYLIC ACIDS AND USES THEREOF
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The present application discloses a compound of formula (I) or a salt thereof: (I) and compositions comprising such compound or salt thereof. The use of such compound, salt thereof or composition comprising same for treating anemia or leukopenia, fibrosis, cancer, hypertension and/or a metabolic condition in a subject is also disclosed.
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- Synthesis of Enantiomerically Enriched 2-Hydroxymethylalkanoic Acids by Oxidative Desymmetrisation of Achiral 1,3-Diols Mediated by Acetobacter aceti
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The stereoselective desymmetrisation of achiral 2-alkyl-1,3-diols is performed by oxidation of one of the two enantiotopic primary alcohol moieties by means of Acetobacter aceti MIM 2000/28 to afford the corresponding chiral 2-hydroxymethyl alkanoic acids (up to 94 % ee). The procedure, carried out in aqueous medium under mild conditions of pH, temperature and pressure, contributes to enlarge the portfolio of enzymatic oxidations available to organic chemists for the development of sustainable manufacturing processes.
- Brenna, Elisabetta,Cannavale, Flavia,Crotti, Michele,De Vitis, Valerio,Gatti, Francesco G.,Migliazza, Gaia,Molinari, Francesco,Parmeggiani, Fabio,Romano, Diego,Santangelo, Sara
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p. 3796 - 3803
(2016/12/24)
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- Synthesis of 3-alkyl(aryl)thietanes
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A preparative procedure for the synthesis of thietanes bearing alkyl substituents in the β-position was developed. Using this procedure, 3-substituted thietanes can be obtained in four steps with an ultimate yield of > 50%. 3-R-thietanes (where R = CH3, C4H9, C5H11, C6H13, C6H 5) and the corresponding sulfoxides and sulfones were synthesized and examined. The feasibility of preparation of gem-3,3-substituted thietanes was exemplified by the synthesis of 3,3-dihexylthietane.
- Shevchenko,Volynskii
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experimental part
p. 123 - 128
(2010/02/28)
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- Mesogenic, optical, and dielectric properties of 5-substituted 2-[12-(4-pentyloxyphenyl)-p-carboran-1-yl] [1,3]dioxanes
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Two homologous series of carborane-containing dioxanes 1[n] and 2[n] (n = 1-10) were prepared and their mesogenic properties investigated. All compounds exhibit nematic behavior and three members of series 2[n] show an E phase. Numerical analysis of the clearing temperatures gave a limiting value T NI(∞) of 89 °C for series 2[n] and indicated conformational flexibility of the dioxane ring. Investigations of three-ring derivative 1[4] gave Δn = 0.17, S = 0.53, and Δε = +0.4 ± 0.1 at 85 °C. Extrapolation of dielectric data for dilute solutions of 1[4] in 6-CHBT gave Δε = +0.4 ± 0.25 at 24 °C. Modelling of dielectric results with the Maier-Meier equation demonstrated that conformers with a higher β angle are preferred, which is consistent with conformational selection for the most elongated conformers. The Royal Society of Chemistry 2006.
- Nagamine, Takashi,Januszko, Adam,Kaszynski, Piotr,Ohta, Kiminori,Endo, Yasuyuki
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p. 3836 - 3843
(2007/10/03)
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- 4-((PHENOXYALKYL)THIO)-PHENOXYACETIC ACIDS AND ANALOGS
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The invention features 4-((phenoxyalkyl)thio)-phenoxyacetic acids and analogs, compositions containing them, and methods of using them as PPAR delta modulators to treat or inhibit the progression of, for example, dyslipidemia.
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Page/Page column 59-60
(2010/02/11)
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- Direct organocatalytic asymmetric α-hydroxymethylation of ketones and aldehydes
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Direct organocatalytic asymmetric α-hydroxymethylation of ketones and aldehydes with formaldehyde has been developed, which furnished the corresponding α-hydroxymethylated adducts with high chemo- and enantioselectivity. The reaction is catalyzed by proline derivatives and is a simple method for the enantioselective synthesis of α-hydroxymethylated ketones and aldehydes, and C-2 symmetric diols.
- Casas, Jesús,Sundén, Henrik,Córdova, Armando
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p. 6117 - 6119
(2007/10/03)
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- The synthesis and electro-optic properties of liquid crystalline 2- (2,3-difluorobiphenyl-4'-yl)-1,3-dioxanes
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Fifty-six novel alkyl and/or alkoxy disubstituted 2-(2,3- difluorobiphenyl-4'-yl)-1,3-dioxanes (DFBPD) were prepared. Smectic C and nematic mesophases were exhibited by most of the alkyl-alkoxy homologues. Conversely, most of the dialkyl compounds exhibited smectic C, smectic A and nematic phases. The birefringence (Δn), dielectric anisotropy (Δε), spontaneous polarisation and response times of two ferroelectric mixtures formulated from the dioxanyl systems were determined. The birefringence results were compared with eight other groups of mixtures where the materials were based on different core systems. The overall electro-optic properties of the DFBPDs were found to be comparable to the best of the eight most commonly used materials in ferroelectric display devices.
- Dong, Chu Chuan,Styring, Peter,Goodby, John W.,Chan, Lawrence K. M.
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p. 1669 - 1677
(2007/10/03)
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- Dioxane derivatives
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Dioxane derivatives for use as components in liquid crystal devices (LCDs) of general formula (A), wherein X is CH or B; R1, R2 are each A1, OA1, OCOA2, or COOA2 ; A1 is a straight or branched chain alkyl group containing from 1 to 20 carbon atoms and may be substituted with one or more F or CN. A2 is a straight or branched chain alkyl group containing from 1 to 20 carbon atoms and may be substituted with one or more F or CN and if straight may be unsubstituted. Y1, Y2, Y3 may each be (CH2)p, (CH2)p COO or OCO(CH2)p ; p is from 0 to 10, n is 0 or 1, m is 0 or 1, either or both of Z1 and Z2 are F and, when not F, are H; Y4 is a covalent bond or, when n is 0, may be (a) LCDs, containing the devices exhibit very fast switching speed, bi-stable characteristics, enhanced greyscale and storage capabilities and a wide viewing angle.
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- 1,3-dioxane derivative and liquid crystal compositions containing it
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A 1,3-dioxane derivative and a liquid crystal composition containing it as expressed by the general formula STR1 (where R is a straight chain alkyl group of carbon number 1 to 10, A is a single bond or --CH2 CH2 -- group, n is 0 or 1, and the cyclohexane ring and 1,3-dioxane ring are respectively in trans form is disclosed.) The 1,3-dioxane derivative represented by general formula (I) has a very large dielectric anisotropy and a small birefringence. Liquid crystal compositions containing (I) can be driven at low voltage and will provide a liquid crystal display apparatus with a wide visual angle.
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- Chemoenzymatic Preparation of Asymmetrized Tris(hydroxymethyl)methane (THYM*) and of Asymmetrized Bis(hydroxymethyl)acetaldehyde (BHYMA*) as New Highly Versatile Chiral Building Blocks
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A series of asymmetrized tris(hydroxymethyl)methanes 2 and bis(hydroxymethyl)acetaldehydes 3 have been prepared in both enantiomeric forms through a chemoenzymatic methodology.The key step is the highly enantioselective PPL-catalyzed monohydrolysis of 2(E)-alkenyl-1,3-diacetoxypropanes 25-27.A careful study on the effect of unsaturations adjacent to the prochiral center in a series of 2-substituted 1,3-diacetoxypropanes has confirmed the suggested beneficial effect of a ? system in that position but has also unveiled an unprecedented dramatic effect of double-bond configuration on enantioselectivity.A new empirical model for the interpretation of these and other results, based both on polarity and steric arguments, is proposed.This study provides a general protocol for the efficient synthesis of asymmetrized 1,3-propanediols bearing in position 2 saturated or unsaturated carbon chains.
- Guanti, Giuseppe,Banfi, Luca,Narisano, Enrica
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p. 1540 - 1554
(2007/10/02)
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- 1,3-dioxane derivatives and composition including same
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2-(3', 4'-difluorophenyl)-1,3-dioxane derivatives represented by the general formula: STR1 wherein R is a linear alkyl group having from 1 to 8 atoms, and having large positive dielectric constant anisotropy (Δε) and small refractive index anisotropy (Δn). The dioxane derivatives may be included in liquid crystal compositions for improved display devices having a low threshold voltage, a low driving voltage and a wide visual angle.
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- Synthesis and Liquid Crystal Properties of Dimethylene Linked Compounds Incorporating the Cyclobutane or Spiroheptane Rings
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The preparation of sixteen dimethylene linked compounds is described heptane ring>, and a comparison is made between the transition temperatures of these compounds and those of the corresponding esters.This comparison once again highlights the fact that the cyclobutane ring should be regarded, in terms of its ability to promote nematic thermal stability, as a "chain stiffener rather than as a ring system.A comparison is also made of the nematic thermal stabilities of the trans-cyclobutane and the spiroheptane systems and of the trans-cyclohexane and the spiroundecane systems.
- Chan, L. K. M.,Gemmell, P. A.,Gray, G. W.,Lacey, D.,Toyne, K. J.
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p. 229 - 246
(2007/10/02)
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- Synthese de l'acide (dimercapto-1,3 propyl-2)-15 pentadecanoique, complexant potentiel du 99mTc
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The synthesis of 15-(1,3-dimercapto 2-propyl) pentadecanoic acid was performed in ten steps.One of these steps is the condensation of (5) with 7-bromoheptanoic acid.It is achieved in liquid ammonia or in a HMPA-THF medium with yields higher than 50 percent.In the second case a-5 bromoacid-ratio of 2.1 (slightly superior to the stoichiometry) is sufficient to obtain these yields, whereas in ammonia, the ratio must be higher than 5 and is therefore clearly unfavourable.The reaction times are also much longer in ammonia.The obtention of 5 from diethyl (6-bromohexyl) malonate 2 implies the reduction of ester functions and the substitution of Br by the ethynyl group.The optimal conditions and the sequence of these two steps have been determined.
- Alagui, Abdelhakim,Apparu, Marcel,Comet, Michel,Pasqualini, Roberto,Vidal, Michel
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p. 113 - 117
(2007/10/02)
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- LIQUID CRYSTAL MATERIALS WITH SULFUR ATOMS INCORPORATED IN THE PRINCIPAL STRUCTURE: 1. NEW LIQUID CRYSTAL COMPOUNDS WITH 1,3-DITHIANE RING.
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2-(p-Substituted phenyl)-5-alkyl-1,3-dithianes, new liquid crystals, were synthesized by the thioacetalization of the corresponding aldehydes and dithiols. These compounds have characteristic supercooling states, exhibit monotropic liquid crystal phases even in the case of long terminal alkyl substituents. The mesomorphic characteristics of these compounds were different from those of the corresponding 1,3-dioxanes, this must originate in the difference in the molecular width caused by the difference in the atomic volume between sulfur and oxygen.
- Haramoto,Nobe,Kamogawa
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p. 1966 - 1969
(2007/10/02)
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- Liquid-crystalline Heterocycloalkanes. I. Synthesis and Properties of Substituted 1,3-Dioxanes
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The synthesis of 2,5-disubstituted 1,3-dioxanes is described, their melting and clearing points and their physical properties (dielectric anisotropy, viscosity, transition enthalpies, optical birefringence) are investigated.The cyano substituted 1,3-dioxanes 5 and 7 are valuable materials for application in displays.
- Vorbrodt, H.-M.,Deresch, S.,Kresse, H.,Wiegeleben, A.,Demus, D.,Zaschke, H.
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p. 902 - 913
(2007/10/02)
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- Research on cyclobutane compounds of biological interest. III. Syntheses and structure activity (antiinflammatory and antalgic) relationships of 3-substituted cyclobutane carboxylic acids
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Antiinflammatory and analgesic activities of 3 substituted cyclobutanecarboxylic acids are pointed out and their structure-activity relationship examined according to the Hansch method. This analysis shows the influence of the steric and lipophilic parameters and this quantitative basis let us realize the synthesis of two acids, the analgesic acitivities of which are very much improved. Attempted quantitative correlations between physiochemical parameters and antiinflammatory activity were unsuccessful. This is imputable to a too imprecise representation of the steric effect which plays a primordial part in this kind of activity.
- Escale,Girard,Vergnon,et al.
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p. 501 - 509
(2007/10/08)
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