- Heterocyclization involving benzylic C(sp3)-H functionalization enabled by visible light photoredox catalysis
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A general and efficient method for heterocyclization involving benzylic C(sp3)-H functionalization enabled by visible light photoredox catalysis to access a wide range of structurally diverse oxygen as well as nitrogen heterocycles up to a gram scale is reported. The potential application of this new methodology is demonstrated by the total synthesis of (-)-codonopsinine and (+)-centrolobine. Herein it is proposed that selectfluor, unlike a fluorinating reagent, acts as an oxidative quencher and a hydrogen radical acceptor.
- Pandey, Ganesh,Laha, Ramkrishna,Mondal, Pradip Kumar
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supporting information
p. 9689 - 9692
(2019/08/15)
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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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- Click-based synthesis and proteomic profiling of lipstatin analogues
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Using click chemistry to enable both structural diversity and proteome profiling within a natural product derived library, two out of nineteen lipstatin analogues showed similar activity to Orlistat against fatty acid synthase (FAS), but with an improved
- Ngai, Mun H.,Yang, Peng-Yu,Liu, Kai,Shen, Yuan,Wenk, Markus R.,Yao, Shao Q.,Lear, Martin J.
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supporting information; experimental part
p. 8335 - 8337
(2010/12/25)
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- Phthalazine derivatives as phosphodiesterase 4 inhibitors
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Compounds of formula (I) wherein B is alkylene, amino, CONH or a bond; Cy is optionally substituted phenyl or heteroaryl; R is H, phenyl or (C1-4)alkyl optionally substituted; R1is (C1-6)alkyl or polyfluoro(C1-6)-alkyl; R2is (C4-7)cycloalkyl optionally containing an oxygen atom and optionally substituted; and the N→O derivatives and pharmaceutically acceptable salt thereof are PDE 4 and TNFα inhibitors.
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- Benzazine derivatives phosphodiesterase 4 inhibitors
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Compounds of formula (I) wherein A is an orthocondensed heterocycle optionally substituted by certain substituents and necessarily substituted by a —B—Cy group where the variables are as defined in the specification and the N→O derivatives and pharmaceutically acceptable salts thereof are phosphodiesterase-4 inhibitors.
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- Insecticidal 5-substituted-2,4-diaminopyrimidine derivatives
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An insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a compound of the formula: STR1 wherein R, R1, R2, R3, R7, R8, m, n, and p are as defined herein, and agriculturally acceptable salts thereof, and methods of using the same.
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