68274-83-9Relevant articles and documents
Synthesis of haminol-A and haminol-B, polyenic alarm pheromones of Cephalaspidean molluscs
Alvarez, Rosana,De Lera, Angel R.
, p. 3065 - 3072 (1998)
Two stereocontrolled palladium-catalyzed cross-couplings of 1-alkenyl boronic acids and aryl/alkenyl halides (the Suzuki-Miyaura reaction) are the key steps in an enantioselective approach to the polyene fragment of haminols A and B, alarm pheromones isolated from Haminoea navicula, a Cephalaspidean Opisthobranch mollusc. Chirality rested on the use of (S)-propylene oxide as the starting material.
2-AMINO-1,3,4-THIADIAZINE AND 2-AMINO-1,3,4-OXADIAZINE BASED ANTIFUNGAL AGENTS
-
Page/Page column 162, (2017/02/09)
The invention provides a compound which is a diazine of formula (I) or a tautomer thereof, or a pharmaceutically acceptable salt thereof, for use as an antifungal agent: (I) wherein X, N', C', A and E are as defined herein. The invention also provides a compound of Formula (I) as defined herein.
Synthesis of triphenylphosphonium Vitamin E derivatives as mitochondria-targeted antioxidants
Jameson, Victoria J.A.,Cochemé, Helena M.,Logan, Angela,Hanton, Lyall R.,Smith, Robin A.J.,Murphy, Michael P.
supporting information, p. 8444 - 8453 (2015/10/12)
A series of mitochondria-targeted antioxidants comprising a lipophilic triphenylphosphonium cation attached to the antioxidant chroman moiety of vitamin E by an alkyl linker have been prepared. The synthesis of a series of mitochondria-targeted vitamin E derivatives with a range of alkyl linkers gave compounds of different hydrophobicities. This work will enable the dependence of antioxidant defence on hydrophobicity to be determined in vivo.
Synthesis of a potent photoreactive acidic γ-secretase modulator for target identification in cells
Rennhack, Andreas,Bulic, Bruno,Jumpertz, Thorsten,Ness, Julia,Baches, Sandra,Weggen, Sascha,Pietrzik, Claus U.
, p. 6523 - 6532,10 (2012/12/12)
Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheimers disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Compounds named γ-secretase modulators (GSMs) can shift the substrate cleavage specificity of γ-secretase toward the production of non-amyloidogenic, shorter Aβ fragments. Herein, we describe the synthesis of highly potent acidic GSMs, equipped with a photoreactive diazirine moiety for photoaffinity labeling. The probes labeled the N-terminal fragment of presenilin (the catalytic subunit of γ-secretase), supporting a mode of action involving binding to γ-secretase. This fundamental step toward the elucidation of the molecular mechanism governing the GSM-induced shift in γ-secretase proteolytic specificity should pave the way for the development of improved drugs against AD.
Synthesis of a potent photoreactive acidic γ-secretase modulator for target identification in cells
Rennhack, Andreas,Jumpertz, Thorsten,Ness, Julia,Baches, Sandra,Pietrzik, Claus U.,Weggen, Sascha,Bulic, Bruno
, p. 6523 - 6532 (2013/01/14)
Supramolecular self-assembly of amyloidogenic peptides is closely associated with numerous pathological conditions. For instance, Alzheime?s disease (AD) is characterized by abundant amyloid plaques originating from the proteolytic cleavage of the amyloid precursor protein (APP) by β- and γ-secretases. Compounds named γ-secretase modulators (GSMs) can shift the substrate cleavage specificity of γ-secretase toward the production of non-amyloidogenic, shorter Aβ fragments. Herein, we describe the synthesis of highly potent acidic GSMs, equipped with a photoreactive diazirine moiety for photoaffinity labeling. The probes labeled the N-terminal fragment of presenilin (the catalytic subunit of γ-secretase), supporting a mode of action involving binding to γ-secretase. This fundamental step toward the elucidation of the molecular mechanism governing the GSM-induced shift in γ-secretase proteolytic specificity should pave the way for the development of improved drugs against AD.
Oxidative cycloaddition of 1,1,3,3-Tetramethyldisiloxane to alkynes catalyzed by supported gold nanoparticles
Lykakis, Ioannis N.,Psyllaki, Androniki,Stratakis, Manolis
supporting information; experimental part, p. 10426 - 10429 (2011/08/05)
Gold nanoparticles supported on TiO2 (0.1-1% mol) catalyze at room temperature and at extremely mild conditions the unprecedented oxidative cycloaddition of 1,1,3,3-tetramethyldisiloxane to alkynes, forming substituted 2,5-dihydro-1,2,5-oxadisiloles, with concomitant evolution of hydrogen gas. For the majority of the substrates, the yields are exceptional (up to 99%). The reaction proceeds at room temperature, tolerates a variety of functional groups, and can be performed in several solvents.
Palladium-catalyzed cascade cyclization of ynamides to azabicycles
Greenaway, Rebecca L.,Campbell, Craig D.,Holton, Oliver T.,Russell, C. Adam,Anderson, Edward A.
supporting information; scheme or table, p. 14366 - 14370 (2012/02/04)
Cascade reactions: A modular assembly of azabicycles by using a cascade cyclization/Suzuki coupling/6π-electrocyclization of bromoenynamides is reported (see scheme). The reaction offers a wide substituent scope on the bicyclic aminodiene products, which can be selectively oxidized as a general approach to aromatic azabicycles.
Sonogashira couplings of aryl bromides: Room temperature, water only, no copper
Lipshutz, Bruce H.,Chung, David W.,Rich, Brian
supporting information; experimental part, p. 3793 - 3796 (2009/07/01)
(Chemical Equation Presented) Cross-coupling reactions between lipophilic terminal alkynes and aryl bromides can be catalyzed by ligated Pd, in the absence of copper, In pure water at ambient temperatures. Small amounts of the nonionic amphiphile PTS assi
TRANSITION METAL COMPLEXES AS LINKERS
-
, (2008/06/13)
The invention relates to new traceless linkers which use transition metal complexes to link a pi-orbital containing substrate for subsequent synthesis by, for example, combinatorial chemistry or multiple parallel synthesis (MPS) to a support.
The application of polymer-bound carbonylcobalt(0) species in linker chemistry and catalysis
Comely, Alex C.,Gibson, Susan E.,Hales, Neil J.,Johnstone, Craig,Stevenazzi, Andrea
, p. 1959 - 1968 (2007/10/03)
Carbonylcobalt(0) species have been used as linkers between alkynes and a polymer support for the first time. The alkynes may be loaded indirectly onto a phosphine functionalised polymer via their hexacarbonyldicobalt(0) complex, or directly onto a cobalt