- Boron Containing PDE4 Inhibitors
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The present invention relates to boron containing compounds of Formula (I) [in-line-formulae]X—Y—Z?? Formula (I)[/in-line-formulae] that inhibit phosphodiesterase 4 (PDE4). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating diseases, conditions, or disorders ameliorated by inhibition of PDE4.
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Paragraph 0759-0760
(2020/04/29)
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- BROMINATED FLAME RETARDANTS AND POLYURETHANES CONTAINING THE SAME
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The disclosure includes brominated alkenyl alcohols, their use as a flame retardant in polyurethane and polyurethane foams, and polyurethanes containing the brominated alkenyl alcohols. Compositions, methods, and processes are disclosed. The brominated alkenyl alcohols used as flame retardants in polyurethanes can be generally described by Formula (I), the scope of which is disclosed herein.
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Paragraph 0122; 0125; 0126; 0159; 0160
(2020/07/15)
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- Steric effects in the design of Co-Schiff base complexes for the catalytic oxidation of lignin models to para-benzoquinones
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New Co-Schiff base complexes that incorporate a sterically hindered ligand and an intramolecular bulky piperazine base in close proximity to the Co center are synthesized. Their utility as catalysts for the oxidation of para-substituted lignin model phenols with molecular oxygen is examined. Syringyl and guaiacyl alcohol, as models of S and G units in lignin, are oxidized in good yield using a catalyst bearing an N-benzylpiperazinyl substituent, with the catalysts displaying improved reactivity for G oxidation. Computational evaluation of the catalysts shows that the piperazinyl substituent is within bonding distance of the Co center. The increased steric interference is suggested as the source of increased G reactivity. This journal is the Partner Organisations 2014.
- Biannic, Berenger,Bozell, Joseph J.,Elder, Thomas
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supporting information
p. 3635 - 3642
(2014/07/08)
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- A simple microwave-assisted preparation of 2-bromo-1-alkenes from 1-alkynes using the LiBr-TMSCl-TEAB reagent system
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2-Bromo-1-alkenes are cleanly and conveniently generated in good yields and selectivities via microwave-assisted hydrobromination of 1-alkynes using a combination of lithium bromide (LiBr), chlorotrimethylsilane (TMSCl), and tetraethylammonium bromide (TEAB) in acetonitrile (MeCN).
- Bunrit, Anon,Ruchirawat, Somsak,Thongsornkleeb, Charnsak
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experimental part
p. 3124 - 3127
(2011/06/26)
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- Concise total syntheses of palominol, dolabellatrienone, β-araneosene, and isoedunol via an enantioselective Diels-Alder macrobicyclization
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Concise total syntheses of four members of the dolabellane family of diterpenoid natural products are reported. Key features of the developed route include the first demonstration of an enantioselective, intramolecular Type I Diels-Alder macrobicyclization, the first example of a stereoselective π-allyl Stille coupling reaction involving a farnesyl-derived intermediate, a powerful new reagent for the formation of dithianes with acid-sensitive molecules, and a unique and highly efficient ring-contraction sequence based on a modified Wolff photochemical rearrangement. Copyright
- Snyder, Scott A.,Corey
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p. 740 - 742
(2007/10/03)
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- Development of aliphatic alcohols as nucleophiles for palladium-catalyzed DYKAT reactions: Total synthesis of (+)-hippospongic acid A
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The ability to use aliphatic alcohols as competent nucleophiles in the palladium-catalyzed dynamic kinetic asymmetric transformation of Baylis-Hillman adducts is explored. High yield and enantioselectivity is obtained for both the kinetic transformation a
- Trost, Barry M.,Machacek, Michelle R.,Tsui, Hong C.
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p. 7014 - 7024
(2007/10/03)
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- NUCLEOBASE PHOSPHONATE ANALOGS FOR ANTIVIRAL TREATMENT
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The present invention provides novel compounds with activity against infectious viruses. The compounds of the invention may inhibit retroviral reverse transcriptases and thus inhibit the replication of the virus. They are useful for treating human patients infected with a human retrovirus, such as human immunodeficiency virus (strains of HIV-1 or HIV-2) or human T-cell leukemia viruses (HTLV-I or HTLV-II) which results in acquired immunodeficiency syndrome (AIDS) and/or related diseases. The present invention also relates generally to the accumulation or retention of therapeutic compounds inside cells. The invention is more particularly related to attaining high concentrations of active metabolite molecules in HIV infected cells. Intracellular targeting may be achieved by methods and compositions which allow accumulation or retention of biologically active agents inside cells. Such effective targeting may be applicable to a variety of therapeutic formulations and procedures.
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Page/Page column 115-116
(2008/06/13)
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- On the regiochemistry of nucleophilic attack on 2-halo π-allyl complexes. 4. The effect of silver acetate and nucleophile concentrations in competitive nucleophilic attack with malonate and phenoxide nucleophiles
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2,3-Dibromo-l-propene or its allyl carbonate analogue are ionized under Pd catalysis to generate the 2-bromo Pd-π-allyl complex (triphenylphosphine ligand), which alkylates with malonate nucleophile at the terminal position. The presence of acetate ion in
- Organ, Michael G.,Arvanitis, Elena A.,Hynes, Stephen J.
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p. 3918 - 3922
(2007/10/03)
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- Syntheses of both enantiomers of 1,7-dioxaspiro[5.5]undecane: Pheromone components of the olive fruit-fly Dacus oleae from a new chiral intermediate, the (S(s))-2-(p-tolylsulfinyl)prop-2-en-1-ol
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Both enantiomers of 1,7-dioxaspiro[5.5]undecane, the pheromone components of the olive fruit-fly Dacus oleae have been synthesized from a new chiral sulfoxide, (Ss)-2-(p-tolylsulfinyl)prop-2-en-1-ol via hetero Diels-Alder reaction, chromatographic separation of the diastereomers on a silica gel column and desulfurization over Raney nickel as key steps.
- Hayes, Patricia,Maignan, Christian
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p. 783 - 786
(2007/10/03)
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- 1,2,2-Tribromocyclopropanecarboxylic acid and derivatives - Valuable intermediates for four carbon cyclopropane and cyclopropene synthons
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Methyl 1,1,2-tribromocyclopropanecarboxylate is readily available by dibromocyclopropanation of methyl α-bromoacrylate. Reaction with methyllithium at low temperature provides a simple route to methyl 2-bromocyclopropene carboxylate, while modification of the ester group followed by reaction with methyllithium leads to a series of related four-carbon cyclopropenes. The tribromo-ester is also readily converted into 1,1,2,2-tetrabromocyclopropane, a valuable three-carbon cyclopropene synthon.
- Al Dulayymi, Ahmad R.,Al Dulayymi, Juma'a R.,Baird, Mark S.,Gerrard, Michelle E.,Koza, Gani,Harkins, Samantha D.,Roberts, Evan
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p. 3409 - 3424
(2007/10/03)
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