- Selective Pd-catalyzed hydrogenation of 3,3-diphenylallyl alcohol: Efficient synthesis of 3,3-diarylpropylamine drugs diisopromine and feniprane
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The Pd-catalyzed selective hydrogenation of C[dbnd]C double bond in (3,3-diphenylallyl)diisopropylamine or 3,3-diphenylallyl alcohol was evaluated using different catalytic systems [Pd/C, Pd(OAc)2/ionic liquid, isolated Pd(0) nanoparticles]. For the (3,3-diphenylallyl)diisopropylamine, hydrogenolysis is preferred over hydrogenation, and only moderate selectivities were obtained for the desired product. However, complete conversion and 100% selectivity were obtained for the hydrogenation of 3,3-diphenylallyl alcohol using isolated Pd(0) nanoparticles under mild condition. This successful strategy enabled the effective synthesis of diisopromine and feniprane drugs and opens new possibilities for the preparation of other biologically active compounds.
- Claudino, Thiago S.,Scholten, Jackson D.,Monteiro, Adriano L.
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- Metal-Free Enantioselective Oxidative Arylation of Alkenes: Hypervalent-Iodine-Promoted Oxidative C?C Bond Formation
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The enantioselective oxyarylation of (E)-6-aryl-1-silyloxylhex-3-ene was achieved using a lactate-based chiral hypervalent iodine(III) reagent in the presence of boron trifluoride diethyl etherate. The silyl ether promotes the oxidative cyclization, and enhances the enantioselectivity. In addition, the corresponding aminoarylation was achieved.
- Shimogaki, Mio,Fujita, Morifumi,Sugimura, Takashi
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p. 15797 - 15801
(2016/12/16)
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- 1,4-dihydropyridine-3,5-dicarboxylate Derivatives And Preparation And Use Thereof
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The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.
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- 1,4-DIHYDROPYRIDINE -3,5-DICARBOXYLATE DERIVATIVES, PREPARATION METHODS AND USES THEREOF
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The present invention relates to a 1,4-dihydropyridine-3,5-dicarboxylate compound of general compound (I), a process for preparing the same, a use thereof for the manufacture of a medicament for treating and/or preventing kidney injury, cardiovascular diseases and/or endocrine diseases, as well as a pharmaceutical composition and a pharmaceutical formulation containing said compounds, wherein the definitions of R1, R2, R3, R4, R5, R6, R7, R8, m, n1, n2, p and q are the same as those defined in the description.
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- Synthesis and evaluation of 4-substituted piperidines and piperazines as balanced affinity μ opioid receptor (MOR) agonist/δ opioid receptor (DOR) antagonist ligands
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In this letter, we describe a series of 4-substituted piperidine and piperazine compounds based on tetrahydroquinoline 1, a compound that shows balanced, low nanomolar binding affinity for the mu opioid receptor (MOR) and the delta opioid receptor (DOR).
- Bender, Aaron M.,Clark, Mary J.,Agius, Michael P.,Traynor, John R.,Mosberg, Henry I.
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supporting information
p. 548 - 551
(2014/01/23)
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- New glucocerebrosidase inhibitors by exploration of chemical diversity of N -substituted aminocyclitols using click chemistry and in situ screening
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A library of aminocyclitols derived from CuAAC reaction between N-propargylaminocyclitol 4 and a series of azides [1′25] is described and tested against GCase. Azides have been chosen from a large collection of potential candidates that has been filtered
- Díaz, Lucía,Casas, Josefina,Bujons, Jordi,Llebaria, Amadeu,Delgado, Antonio
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supporting information; experimental part
p. 2069 - 2079
(2011/06/10)
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- 2H-PYRAZOLO [4,3-D]PYRIMIDIN-5-AMINE DERIVATIVES AS H4 HISTAMINE RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ALLERGIC, IMMUNOLOGICAL AND INFLAMMATORY DISEASES
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Pyrazolopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.
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Page/Page column 100-101
(2010/04/30)
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- MALE CONTRACEPTIVE
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A compound having formula (I). R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, a
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Page/Page column 18
(2008/12/07)
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- N-3(9)-arylpropenyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes as μ-opioid receptor agonists. Effects on μ-affinity of arylalkenyl chain modifications
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Two series of N-3-arylpropenyl-N-9-propionyl-3,9-diazabicyclo[3.3.1]nonanes (1b-j) and of the reverted N-3-propionyl-N-9-arylpropenyl isomers (2b-j) as analogues of the previously reported analgesic N-3(9)-cinnamyl-N-9(3)-propionyl-3,9-diazabicyclo[3.3.1]nonanes (DBN) (1a, 2a) were synthesised and their affinity and selectivity towards opioid μ-, δ- and κ-receptors were evaluated. Several compounds (1e,i,j-2d,e,f,g,j) exhibited a μ-affinity in the low nanomolar range with moderate or negligible affinity towards δ- and κ-receptors. The representative term N-9-(3,3-diphenylprop-2-enyl)-N-3-propionyl-DBN (2d) displayed in vivo (mouse) a potent analgesic effect (ED50 3.88 mg/kg ip) which favourably compared with that of morphine (ED50 5 mg/kg ip). In addition, 2d produced in mice tolerance after a period twice as long with morphine.
- Pinna, Gérard A.,Cignarella, Giorgio,Loriga, Giovanni,Murineddu, Gabriele,Mussinu, Jean-Mario,Ruiu, Stefania,Fadda, Paola,Fratta, Walter
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p. 1929 - 1937
(2007/10/03)
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- Tricyclic compounds, their production and use
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A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N= or —C(R3)= (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.
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