Top Picks: new discover of 6,7-Dimethoxy-1,2,3,4-tetrahydroisoquinoline

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NOVEL TETRAHYDROISOQUINOLINE COMPOUNDS FOR USE IN THE DIAGNOSIS AND TREATMENT OF NEURODEGENERATIVE DISEASES

The invention relates to a new class of compounds with high affinity and selectivity towards P-glycoprotein. The invention also relates to the utilization of such compounds in the in vivo diagnosis of neurodegenerative diseases and as medicaments for use in the prevention and treatment of neurodegenerative disease involving P-glycoprotein.

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

The Absolute Best Science Experiment for 7-Nitro-1,2,3,4-tetrahydroisoquinoline

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Exploring the active site of phenylethanolamine N-methyltransferase with 1,2,3,4-tetrahydrobenz[h]isoquinoline inhibitors

1,2,3,4-Tetrahydrobenz[h]isoquinoline (THBQ, 11) is a potent, inhibitor of phenylethanolamine N-methyltransferase (PNMT). Docking studies indicated that the enhanced PNMT inhibitory potency of 11 (hPNMT Ki = 0.49 muM) versus 1,2,3,4-tetrahydroisoquinoline (5, hPNMT Ki = 5.8 muM) was likely due to hydrophobic interactions with Val53, Met258, Val272, and Val269 in the PNMT active site. These studies also suggested that the addition of substituents to the 7-position of 11 that are capable of forming hydrogen bonds to the enzyme could lead to compounds (14-18) having enhanced PNMT inhibitory potency. However, these compounds are in fact less potent at PNMT than 11. Furthermore, 7-bromo-THBQ (19, hPNMT Ki = 0.22 mM), which has a lipophilic 7-substituent that cannot hydrogen bond to the enzyme, is twice as potent at PNMT than 11. This once again illustrates the limitations of docking studies for lead optimization.

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

Can You Really Do Chemisty Experiments About 17680-55-6

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Mn(II)-Catalyzed N -Acylation of Amines

A practical protocol has been developed here for the Mn(II)-catalyzed N -acylation of amines with high yields using N, N -dimethylformamide and other amides as the carbonyl source. The protocol is simple, does not require any acid, base, ligand, or other additives, and encompasses a broad substrate scope for primary, secondary, and heterocyclic amines.

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

Discovery of 118864-75-8

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In homogeneous catalysis, the catalyst is in the same phase as the reactant. The number of collisions between reactants and catalyst is at a maximum.In a patent, 118864-75-8, name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline, introducing its new discovery. Formula: C15H15N

Stereoselective Total Syntheses of Solifenacin and N -Acetyl-1-(4-chloro-phenyl)-6,7-dimethoxytetrahydroisoquinoline

A highly stereoselective synthesis of 1-aryl-1,2,3,4-tetrahydroisoquinoline drugs such as solefinacin (muscarinic acetylcholine receptor antagonist) and N-acetyl-1-(4-chlorophenyl)-6,7-dimethoxytetrahydroisoquinoline (AMPA receptor antagonist) has been accomplished using (R)-tert-butanesulfinamide as a chiral source. Chiral tetrahydroisoquinolines have been prepared through the aryl Grignard addition to chiral N-sulfinylimines followed by haloamide cyclization.

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

New explortion of 1745-07-9

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Electrochemical Approach for Direct C-H Phosphonylation of Unprotected Secondary Amine

Direct alpha-phosphonylation of an unprotected secondary amine in a single step is of practical importance to amino phophophates. However, this protocol is limited due to the high redox barrier of unprotected amine. In this paper, we report C-H phosphonylation of an unprotected secondary amine via an electrochemical approach in the presence of catalytic carboxylate salt. This metal-free and exogenous oxidant-free method furnishes diverse target molecules with satisfactory yield under mild reaction conditions. Successful application of the protocol in a gram-scale experiment demonstrates the potential utility for further functionalization.

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

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

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Visible-light-induced direct alpha-C(sp3)-H thiocyanation of tertiary amines

Visible-light-induced, eosin Y catalyzed aerobic oxidative alpha-C(sp3)-H thiocyanation of tertiary amines is reported. The reaction proceeds through visible-light-induced in situ generation of the iminium ion followed by attack of -SCN nucleophile. This is the first example of visible-light-initiated formation of C(sp3)-S bond employing organo-photoredox catalysis. Mild reaction conditions and use of air and visible light as the greenest and sustainable reagents at room temperature are the salient features of the protocol.

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

More research is needed about 118864-75-8

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Process for preparing polymorphic forms of solifenacin succinate

Polymorphic forms of solifenacin have been prepared and characterized. These polymorphic forms are particularly useful in pharmaceutical compositions.

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

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

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Photoredox catalytic organic reactions promoted with broadband visible light-absorbing Bodipy-iodo-aza-Bodipy triad photocatalyst

The 4-bora-3a,4a-diaza-s-indacene scaffold is known as Bodipy. 2,6-Diiodo-aza-Bodipy (B-1) and the Bodipy-2,6-diiodo-aza-Bodipy triad (B-2) have been used as novel photocatalysts for photoredox catalytic organic reactions with tetrahydroisoquiniline as substrate to prepare highly functionalized organic compounds via a [3 + 2] cycloaddition-aromatization tandem reaction and Cu(i)-catalyzed alkynylation reactions. In distinction to conventional photocatalysts such as Ru(bpy)3Cl2, Eosin Y or Rose Bengal, which are based on a mono-visible light-harvesting chromophore profile and show weak absorption in the visible region, the new photocatalysts are strong visible absorbers (B-1, epsilon = 73000 M-1 cm-1 at 683 nm). More importantly, resonance energy transfer (RET) has been used to increase the absorption of photocatalyst B-2 in the visible region, in which two Bodipy units were used as energy donor and diiodo-aza-Bodipy as energy acceptor. B-2 shows broadband absorption in the range 400-750 nm (epsilon = 165 000 M-1 cm-1 at 504 nm, and 71000 M-1 cm -1 at 683 nm). Iodo-aza-Bodipy is more efficient than conventional photocatalysts such as [Ru(bpy)3]Cl2. Furthermore, the broadband visible light-absorbing B-2 is more efficient as a photocatalyst than previously reported monochromophore photocatalyst B-4 (diiodo-Bodipy). Our results will be useful for the design of efficient organic triplet photosensitizers as photocatalysts for photoredox catalytic organic reactions. This journal is the Partner Organisations 2014.

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

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The singlet excited state of BODIPY promoted aerobic cross-dehydrogenative-coupling reactions under visible light

In contrast to previous studies, we disclose for the first time that the singlet excited state (1PS?) of BODIPY rather than the triplet excited state (3PS?) can drive C-H bond activation to form C-C and C-P bonds smoothly, which offers new methods to promote organic transformation under visible light irradiation.

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

Archives for Chemistry Experiments of 1-Phenyl-1,2,3,4-tetrahydroisoquinoline

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Solvent to promote tetrahydroisoquinoline compound selective dehydrogenation method (by machine translation)

A solvent the promotion of the 1 – substituted – 1, 2, 3, 4 – tetrahydroisoquinoline compound selective partial dehydrogenation synthesis of 1 – substituted – 3, 4 – ISO-quinoline. For the simple and easily obtained cyclic amine compound such as tetrahydroisoquinoline compounds, can be through selective dehydrogenation to obtain the corresponding imine compound, its conversion rate is high, and part of the dehydrogenation product and fully dehydrogenation product of the proportion is more than 20:1. The operation of the invention is simple and practical and easy, mild reaction conditions, the actual cost is greatly reduced. In addition, through the tetrahydroisoquinoline direct dehydrogenation synthesis of 3, 4 – ISO-quinoline method, with the atom economy, friendly advantage of the environment. (by machine translation)

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