- Tris(pyrazolyl)borate Copper Hydroxide Complexes Featuring Tunable Intramolecular H-Bonding
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A modular synthesis provides access to a series of new tris(pyrazolyl)borate ligands XpyMeTpK that possess a single functionalized pendant pyridyl (py) or pyrimidyl (pyd) arm designed to engage in tunable intramolecular H-bonding to metal-bound functionalities. To illustrate such H-bonding interactions, a series of [XpyMeTpCu]2(μ-OH)2 (6a-6e) complexes were synthesized from the corresponding XpyMeTpCu-OAc (5a-5e) complexes. Single crystal X-ray structures of three new dinuclear [XpyMeTpCu]2(μ-OH)2 complexes reveal H-bonding between the pendant heterocycle and bridging hydroxide ligands while the donor arm engages the copper center in an unusual monomeric DMAPMeTpCu-OH complex. Vibrational studies (IR) of each bridging hydroxide complex reveal reduced νOH frequencies that tracks with the H-bond accepting ability of the pendant arm. Reversible protonation studies that interconvert [XpyMeTpCu]2(μ-OH)2 and [XpyMeTpCu(OH2)]OTf species indicate that the acidity of the corresponding aquo ligand decreases with increasing H-bond accepting ability of the pendant arm.
- Gardner, Evan J.,Cobb, Caitlyn R.,Bertke, Jeffery A.,Warren, Timothy H.
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- Synthesis of Esters by Functionalisation of CO2
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The invention relates to a method for (I) producing a carboxylic ester of formula (I). Said method comprises the steps of: a) bringing an organosilane/borane of formula Si or B into contact with CO2, in the presence of a catalyst and an electrophilic compound of formula (III), the groups R1, R2, R3, R4, R5, Y, and M′ being as defined in claim 1; and optionally b) recovering the compound of formula (I) produced.
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Paragraph 0129
(2017/09/06)
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- AMIDE COMPOUND OR SALT THEREOF, AGRICULTURAL AND HORTICULTURAL INSECTICIDE AND MICROBICIDE COMPRISING THE COMPOUND, AND METHOD FOR USING THE INSECTICIDE AND MICROBICIDE
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In crop production in the fields of agriculture, horticulture, and the like, the damage caused by insect pests etc. is still immense, and insect pests resistant to existing insecticides have emerged. Under such circumstances, the development of novel agricultural and horticultural insecticides is desired. The present invention, provides an amide compound represented by the general formula (I): (wherein A1, A2 and A3 each represent a nitrogen atom or a CH group, R1 represents an alkyl group, R2 and R4 each represent a haloalkyl groups, R3 represents an alkyl group, and m represents 0, 1 or 2) or a salt thereof; an agricultural and horticultural insecticide and microbicide comprising the compound or a salt thereof as an active ingredient; and a method for using the insecticide and microbicide.
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Paragraph 0150; 0151
(2017/04/15)
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- CO2 Conversion into Esters by Fluoride-Mediated Carboxylation of Organosilanes and Halide Derivatives
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A one-step conversion of CO2 into heteroaromatic esters is presented under metal-free conditions. Using fluoride anions as promoters for the C-Si bond activation, pyridyl, furanyl, and thienyl organosilanes are successfully carboxylated with CO2 in the presence of an electrophile. The mechanism of this unprecedented reaction has been elucidated based on experimental and computational results, which show a unique catalytic influence of CO2 in the C-Si bond activation of pyridylsilanes. The methodology is applied to 18 different esters, and it has enabled the incorporation of CO2 into a polyester material for the first time. Metal free! A novel methodology is described to convert CO2 into heteroaromatic esters in the presence of organosilanes and organic halides using fluoride anions as promoters for the C-Si bond activation (see scheme). CO2 exhibits a unique catalytic influence in the C-Si bond cleavage of pyridylsilanes, serving as a traceless activator.
- Frogneux, Xavier,Von Wolff, Niklas,Thuéry, Pierre,Lefèvre, Guillaume,Cantat, Thibault
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p. 2930 - 2934
(2016/03/25)
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- Iminothiadiazine Dioxide Compounds as BACE Inhibitors, Compositions and Their Use
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In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.
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Paragraph 0563
(2015/11/16)
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- NOVEL PYRIDINE DERIVATIVES
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The invention relates to a compound of formula (I) wherein R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 61; 62
(2014/06/24)
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- THIAZALOPYRROLIDINE INHIBITORS OF ROR-GAMMA
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Provided are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR?. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.
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Paragraph 00172
(2014/11/13)
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- 1-(DIHYDRONAPHTHALENYL)PYRIDONES AS MELANIN-CONCENTRATING HORMONE RECEPTOR 1 ANTAGONISTS
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This invention relates to novel 1-(dihydronaphthalenyl)pyridones which are antagonists of the melanin-concentrating hormone receptor 1 (MCHR1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy
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Page/Page column 48
(2013/12/03)
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- NOVEL PYRIDINE DERIVATIVES
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The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 76
(2013/02/27)
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- PYRIDIN- 2 -AMIDES USEFUL AS CB2 AGONISTS
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The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
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Page/Page column 158; 159
(2013/02/27)
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- TRPV1 ANTAGONISTS
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Compounds of formula (I) wherein R1, R2, R4, and W are defined in the description are TRPV 1 antagonists with CNS penetration. Compositions comprising such compounds and methods for treating conditions and disorders using
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Page/Page column 25
(2009/05/28)
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