Extracurricular laboratory:new discovery of (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline

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Discovery of a 1-isopropyltetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain

N-type calcium channel blockade is a promising therapeutic approach for the treatment of neuropathic pain. Starting from lead compound (S)-1, we focused our optimization efforts on potency for N-type calcium channel inhibition and improvement of CYP inhibition profile. 2-{[(1-Hydroxycyclohexyl)methyl]amino}-(1R)-(1-isopropyl-6-methoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethanone oxalate ((R)-5r) was identified as a novel orally active small-molecule N-type calcium channel inhibitor with reduced CYP inhibition liability. Oral administration of (R)-5r improved mechanical allodynia in a spinal nerve ligation model of neuropathic pain in rats with an ED50 value of 2.5 mg/kg.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Carbon nitride-catalyzed photoredox C-C bond formation with N-aryltetrahydroisoquinolines

In this communication we describe the oxidative C-C bond formation of tertiary amines with various nucleophiles under very mild and environmental friendly conditions by using mesoporous graphitic carbon nitride (mpg-C 3N4) semiconductor as a heterogeneous, metal-free photosensitizer in combination with visible light and oxygen as the terminal oxidation agent. This system can be further combined with proline- organocatalysis to achieve oxidative tandem photocatalysis, demonstrating a rich cascade of chemical possibilities of the current photosynthesis system. Copyright

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

A new application about 6-Bromo-1,2,3,4-tetrahydroisoquinoline

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Discovery of a brain-penetrant S1P3-sparing direct agonist of the S1P1 and S1P5 receptors efficacious at low oral dose

2-Amino-2-(4-octylphenethyl)propane-1,3-diol 1 (fingolimod, FTY720) has been recently marketed in the United States for the treatment of patients with remitting relapsing multiple sclerosis (RRMS). Its efficacy has been primarily linked to the agonism on T cells of S1P1, one of the five sphingosine 1-phosphate (S1P) G-protein-coupled receptors, while its cardiovascular side effects have been associated with activity at S1P3. Emerging data suggest that the ability of this molecule to cross the blood-brain barrier and to interact with both S1P1 and S1P5 in the central nervous system (CNS) may contribute to its efficacy in treating patients with RRMS. We have recently disclosed the structure of an advanced, first generation S1P 3-sparing S1P1 agonist, a zwitterion with limited CNS exposure. In this Article, we highlight our strategy toward the identification of CNS-penetrant S1P3-sparing S1P1 and S1P5 agonists resulting in the discovery of 5-(3-{2-[2-hydroxy-1-(hydroxymethyl) ethyl]-5-methyl-1,2,3,4-tetrahydro-6-isoquinolinyl}-1,2,4-oxadiazol-5-yl) -2-[(1-methylethyl)oxy]benzonitrile 15. Its exceptional in vivo potency and good pharmacokinetic properties translate into a very low predicted therapeutic dose in human (<1 mg p.o. once daily). If you are interested in 226942-29-6, you can contact me at any time and look forward to more communication. category: tetrahydroisoquinoline

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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A activation containing C – H bond in the compound of C – H key method and its application (by machine translation)

The invention discloses an activating compound containing C – H bond in C – H of the key of the method, the method comprises: inert gas protection and visible light irradiation, containing the photocatalyst and solvent in the system, adding containing C – H compound of the key, the photocatalyst is a quantum dot. The invention also discloses a key compound containing C – H of the C – H bond functionalized method, the method comprises: inert gas protection and visible light irradiation, containing the photocatalyst and solvent in the system, adding containing C – H compound of the key, the photocatalyst for the quantum dot, and containing C – H to the compound of the key in the key functionalized C – H. The invention under protection of inert gas, by using visible light irradiation, realizing C – H key activation and alkene third functionalization of the C – H bond. The invention quantum dot as a photocatalyst, mild reaction conditions, without the participation of the oxidizing agent, the atom economy, catalyst can be reused. (by machine translation)

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Extracurricular laboratory:new discovery of 6-Bromo-1,2,3,4-tetrahydroisoquinoline

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MODULATORS OF THE HISTAMINE H3 RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO

Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer”s disease, pain and the like.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

The Absolute Best Science Experiment for 149353-95-7

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SUBSTITUTED SPIROAMIDE COMPOUNDS

Substituted spiroamide compounds corresponding to formula (I): wherein A, B, Q1, Q2, Q3, Q4, R1, R8, R9a, R9b, R12, R13, R200 and R210 have defined meanings, processes for their preparation, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting pain or other conditions mediated at least in part by the bradykinin 1 receptor (B1R)

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Extended knowledge of 1-Phenyl-1,2,3,4-tetrahydroisoquinoline

The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 22990-19-8 is helpful to your research. Related Products of 22990-19-8

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A PROCESS FOR THE PREPARATION OF SOLIFENACIN SALTS AND THEIR INCLUSION INTO PHARMACEUTICAL DOSAGE FORMS

The invention relates to the synthesis of solifenacin, the preparation of its salts and their inclusion into pharmaceutically acceptable dosage forms.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Top Picks: new discover of 1-Phenyl-1,2,3,4-tetrahydroisoquinoline

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Process for the preparation of solifenacin

A process for the preparation of (1S,3’R)-quinielidin-3′-yl-1-phenyl-3,4-dihydro-1H-isoquinolin-2-carboxylate, namely solifenacin, comprising the reaction of a compound of formula (IV) with a compound of formula (V), as herein defined, and the subsequent reaction with 3-quinuclidinol.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

Discovery of 2-Phenyl-1,2,3,4-tetrahydroisoquinoline

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TiO2 Nanoparticles Functionalized with Non-innocent Ligands Allow Oxidative Photocyanation of Amines with Visible/Near-Infrared Photons

Photosynthesis is an efficient mechanism for converting solar light energy into chemical energy. We report on a strategy for the aerobic photocyanation of tertiary amines with visible and near-infrared (NIR) light. Panchromatic sensitization was achieved by functionalizing TiO2 with a 2-methylisoquinolinium chromophore, which captures essential features of the extended ?-system of 2,7-diazapyrenium (DAP2+) dications or graphitic carbon nitride. Two phenolic hydroxy groups make this ligand highly redox-active and allow for efficient surface binding and enhanced electron transfer to the TiO2 surface. Non-innocent ligands have energetically accessible levels that allow redox reactions to change their charge state. Thus, the conduction band is sufficiently high to allow photochemical reduction of molecular oxygen, even with NIR light. The catalytic performance (up to 90% chemical yield for NIR excitation) of this panchromatic photocatalyst is superior to that of all photocatalysts known thus far, enabling oxidative cyanation reactions to the corresponding alpha-cyanated amines to proceed with high efficiency. The discovery that the surface-binding of redox-active ligands exhibits enhanced light-harvesting in the red and NIR region opens up the way to improve the overall yields in heterogeneous photocatalytic reactions. Thus, this class of functionalized semiconductors provides the basis for the design of new photocatalysts containing non-innocent donor ligands. This should increase the molar extinction coefficient, permitting a reduction of nanoparticle catalyst concentration and an increase of the chemical yields in photocatalytic reactions.

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Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem

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Preparation of amides and quinazoline derivatives

The present invention relates to a process for the preparation of amides, comprising reacting amines with carboxylic acids in the presence of silicon amines. The present invention further relates to a process for the preparation of quinazoline derivatives, comprising reacting amines with carboxylic acids in the presence of silicon amines to obtain amides and contacting the resultant amides with quinazoline.

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Reference£º
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem