The Absolute Best Science Experiment for N1,N2-Di-tert-butylethane-1,2-diamine

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A highly enantioselective gold(I)-catalyzed intermolecular tandem cyclization/[3 + 2] cycloaddition of 2-(1-alkynyl)-2-alken-1-ones with 3-stylindoles was achieved by using Ming-Phos as a chiral ligand. A variety of chiral highly substituted cyclopenta[c]furans were obtained in good yields (up to 99%) with excellent diastereoselectivities (>20:1) and enantioselectivities (up to 97% ee). The salient features of the present protocol include mild conditions, excellent yields, and high diastereo- and enantioselectivities, using readily available starting materials and a chiral ligand.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention relates to a new process for the preparation of compound of general formula (I) which is the inhibitor of Purine Nucleoside phosphorylase (PNP), purine phosphoribosyltransferase (PPRT), 5′-methylthioadenosine phosphorylase (MTAP), 5′-methylthioadenosine nucleosidase (MTAN) and/or nucleoside hydrolase (NH).The present invention relates to a new process for the preparation of compound of general formula (I) which is the inhibitor of purine nucleoside phosphorylase (PNP), purine phosphoribosyltransferase (PPRT), 5′-methylthioadenosine phosphorylase (MTAP), 5′ methylthioadenosine nucleosidase (MTAN) and/or nucleoside hydrolase (NH)

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The synthesis and utility of novel indole-olefin-oxazoline (IndOlefOx)-ligands are described. The use of these ligands was demonstrated in rhodium catalyzed asymmetric conjugate additions between 2-cyclopentenone, 2-cyclohexenone, and 2-cycloheptenone with different boron reagents with good yields and enantioselectivities of up to 94%.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The total synthesis of a potential inhibitor of HIV-protease-the chiral nonracemic six-membered hydroxy lactam 6-has been accomplished, that involves, as key reaction, the highly diastereoselective vinylogous Mannich addition of furan-based silyloxy diene 7 to glyceraldeyde imine 8.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Silver complexes [Ph3PCH2CH2PPh3]2+[Ag2Cl4]2? (I), [Ph3PCH2OCH3]2 +[Ag2Cl4]2- (II), [Ph3P(i-Am)]2 +[Ag2Br4]2- (III), [Ph3PC6H11-cyclo]2 +[Ag2Br4]2- (IV), [Ph3PCH2Ph]2 +[Ag2Br4]2- (V), [Ph3PCH = CH2]n +[Ag2Br3]n – (VII) have been synthesized by the reaction between tetraorganylphosphonium halides and silver chloride or silver bromide in dimethylsulfoxide. According to X-ray diffraction data, the ionic complexes are built of tetraorganylphosphonium cations and binuclear (I?V) or polynuclear (VI, VII) anions. In the anions of complexes VI and VII, silver atoms are tetracoordinated, and bromine atoms have coordination numbers of 2 and 4.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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The Wittig reaction of 1-acetyl-2-methoxy- (1) and 1-acetyl-2-hydroxyindol-3(2H)-one (2) with stabilized and semistabilized ylides gave predominantly 3-alkylidenedihydroindoles (4), (7), and (13) with (Z)-stereochemistry.When the Wittig reaction was carried out under more drastic conditions, the Wittig products (4) and (7) isomerized to afford 3-alkylindoles (5) and the indol-2-one (8), respectivily.These isomerizations are also described.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Irradiation of terminal aromatic gamma,delta-epoxy ketones with a 450 W UV lamp led to Norrish type II cyclization/semi-pinacol rearrangement cascade reaction which formed the benzocyclobutanones containing a full-carbon quaternary center, whereas irradiation of substituted aromatic gamma,delta-epoxy ketones led to the indanones through a photochemical epoxy rearrangement and 1,5-biradicals cyclization tandem reaction.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an alpha5-containing GABAA receptor agonist (e.g., an alpha5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer’s Disease(AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson’s disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an alpha5-containing GABAA receptor agonist (e.g., an alpha5-containing GABAA receptor positive allosteric modulator) in treating brain cancers (including brain tumors, e.g., medulloblastomas), and cognitive impairment associated therewith.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI

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Photolysis of regioisomeric helical chromenes 1 and 2 leads to colored reactive intermediates. While the latter generally decay quite rapidly, they are found to be longer lived in 1 and highly persistent in 2. The remarkable stability of the otherwise fleeting transient in 2 allowed isolation and structural characterization by X-ray crystallography. The structural analyses revealed that steric force inherent to the helical scaffold is the origin of stability as well as differentiation in the persistence of the intermediates of 1 and 2 (1Q and 2Q). The structure further shows that diphenylvinyl moiety in the TT isomer of 2Q gets splayed over the helical scaffold such that it is fraught with a huge steric strain to undergo required bond rotations to regenerate the precursor chromene. Otherwise, reversion of 2Q was found to occur at higher temperatures. Aazahelical chromenes 3 and 4 with varying magnitudes of helicity were designed in pursuit of o-quinonoid intermediates with graded activation barriers. Their photogenerated intermediates 3Q and 4Q were also isolated and structurally characterized. The activation barriers for thermal reversion of 2Q-4Q, as determined from Arrhenius and Eyring plots, are found to correlate nicely with the helical turn, which decisively determines the steric force. The exploitation of helicity is thus demonstrated to develop a novel set of photoresponsive helicenes 2-4 that lead to colored intermediates exhibiting graded stability. It is further shown that the photochromism of 2-4 in conjunction with response of 2Q-4Q to external stimuli (acid, heat, and visible radiation) permits development of molecular logic gates with INHIBIT function.

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Reference:
Metal catalyst and ligand design,
Ligand Template Strategies for Catalyst Encapsulation – NCBI