Category: 118864-75-8

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. name: (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline

Process for the Synthesis of Solifenacin

This invention provides improved methods for making solifenacin and pharmaceutically acceptable salts thereof. The instant methods are unexpectedly advantageous in their simplicity and efficiency.

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

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. Computed Properties of C15H15N

Discovery of an 8-methoxytetrahydroisoquinoline derivative as an orally active N-type calcium channel blocker for neuropathic pain without CYP inhibition liability

In lead optimization efforts starting from the tetrahydroisoquinoline (S)-1, we identified 2-{[(2R)-2-hydroxypropyl]amino}-1-[(1S)-8-methoxy-1-phenyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone ((1S)-8t) as a novel orally active small-molecule N-type calcium channel blocker without CYP inhibition liability. CYP3A4 inhibition profile was improved by reducing the lipophilicity of compound (S)-1. Moreover, introduction of a methoxy group to the C-8 position of tetrahydroisoquinoline led to identification of (1S)-8t, which eliminated CYP2D6 inhibition liability. Oral administration of (1S)-8t exerted efficacy in a rat spinal nerve ligation (SNL) model of neuropathic pain with an ED50 value of 2.8 mg/kg.

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

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Computed Properties of C15H15N, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 118864-75-8, name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline. In an article£¬Which mentioned a new discovery about 118864-75-8

A new thorley that and the post-treatment of new thorley that method of producing succinic acid (by machine translation)

The invention discloses a method of post-processing of the new thorley that, including the synthesis of new thorley thattotal fluid dropping slowly in strengthening acid, adjusting the pH value to 1.0-2.0 temperature after, add water using the extractant; after lowering the aqueous phase by adding saturated sodium carbonate solution to the alkaline, then adding dichloromethane sub-time extraction, extract use of water washing, by adding desiccant drying, position of; the evaporation in the low temperature position to the oily substance solly that our novel alkali. This invention, through optimization of the post-treatment process, the alkali treatment process after new thorley that steps in the use of only two kinds of solvent ISO-propyl ether and dichloromethane, type of the solvent is reduced, it is easy to operate and recycled, the cost is greatly saved. In the hydrochloric acid solly the new return alkali process are not used in a strong base or strong acid, using the saturated NaCO3 solution, the reaction is more moderate, is beneficial to control the temperature, the more important thing is the generation of the isomer is greatly reduced, so that the non-(1S, 3R) isomer of a reduced content of configuration. (by machine translation)

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

Electric Literature of 118864-75-8, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline,introducing its new discovery.

Engineering an enantioselective amine oxidase for the synthesis of pharmaceutical building blocks and alkaloid natural products

The development of cost-effective and sustainable catalytic methods for the production of enantiomerically pure chiral amines is a key challenge facing the pharmaceutical and fine chemical industries. This challenge is highlighted by the estimate that 40-45% of drug candidates contain a chiral amine, fueling a demand for broadly applicable synthetic methods that deliver target structures in high yield and enantiomeric excess. Herein we describe the development and application of a “toolbox” of monoamine oxidase variants from Aspergillus niger (MAO-N) which display remarkable substrate scope and tolerance for sterically demanding motifs, including a new variant, which exhibits high activity and enantioselectivity toward substrates containing the aminodiphenylmethane (benzhydrylamine) template. By combining rational structure-guided engineering with high-throughput screening, it has been possible to expand the substrate scope of MAO-N to accommodate amine substrates containing bulky aryl substituents. These engineered MAO-N biocatalysts have been applied in deracemization reactions for the efficient asymmetric synthesis of the generic active pharmaceutical ingredients Solifenacin and Levocetirizine as well as the natural products (R)-coniine, (R)-eleagnine, and (R)-leptaflorine. We also report a novel MAO-N mediated asymmetric oxidative Pictet-Spengler approach to the synthesis of (R)-harmicine.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, category: tetrahydroisoquinoline, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C15H15N

Asymmetric synthesis and enantioselectivity of binding of 1-aryl-1,2,3,4-tetrahydroisoquinolines at the PCP site of the NMDA receptor complex

A new method for the asymmetric synthesis of 1-substituted tetrahydroisoquinolines is presented. It is based on stereoselective addition reactions of organometallic compounds to the intermediate N-acylimimum ion 6, which is provided with an N-acyl group as a chiral auxiliary. In addition reactions with organomagnesium and organozinc reagents diastereoselectivities from 70:30 to 95:5 (for 7/8) were observed with the zinc reagents in general leading to markedly improved stereoselectivities. By catalytic hydrogenation of 7 and 8 and after removal of the chiral auxiliary the target compounds 11 and 12 were obtained. The enantiomerically pure 11c-g and 12c-g (ee > 99%), 1-aryltetrahydroisoquinolines, were evaluated for their affinity to the PCP [1-(1-phenylcyclohexyl)piperidine] binding site of the NMDA (N-methyl D-aspartate) receptor. In each case the enantiomers 11 exhibited a higher affinity than those of 12, with the potencies of the enantiomers differing by a factor of 4 (11/12g) to 27 (11/12c). The absolute configuration of the more potent enantiomers 11 is in accordance with the stereochemical requirement found for FR 115427 (3) which is a close analogue.

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

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One-Pot N-Deprotection and Catalytic Intramolecular Asymmetric Reductive Amination for the Synthesis of Tetrahydroisoquinolines

A one-pot N-Boc deprotection and catalytic intramolecular reductive amination protocol for the preparation of enantiomerically pure tetrahydroisoquinoline alkaloids is described. The iodine-bridged dimeric iridium complexes displayed superb stereoselectivity to give tetrahydroisoquinolines, including several key pharmaceutical drug intermediates, in excellent yields under mild reaction conditions. Three additives played important roles in this reaction: Titanium(IV) isopropoxide and molecular iodine accelerated the transformation of the intermediate imine to the tetrahydroisoquinoline product; p-toluenesulfonic acid contributed to the stereocontrol.

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

Related Products of 118864-75-8, Chemistry is the experimental science by definition. We want to make observations to prove hypothesis. For this purpose, we perform experiments in the lab. 118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline,introducing its new discovery.

Method for preparing chiral amine compound and its application (by machine translation)

The invention discloses a preparation method of a chiral amine compound. In presence of a semi-sandwich type complex and an acid additive, an asymmetrization reaction is carried out on a prochiral amine compound in a hydrogen atmosphere, and postprocessing is carried out after the reaction is completely finished, so that the chiral amine compound is obtained. According to the preparation method of the chiral amine compound, a certain amount of appropriate acid is added in a certain sequence, so that activation of a C=N bond in a reduction reaction can be promoted; the prepared chiral amine compound can be taken as an intermediate and used for synthesizing the following medicines (including but not limited to the medicines) or precursors of the medicines: gantacurium, mivacurium chloride, atracurium besylate, sertraline, sezolamide, almorexant or solifenacin.

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

Application of 118864-75-8, Because a catalyst decreases the height of the energy barrier, its presence increases the reaction rates of both the forward and the reverse reactions by the same amount.118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C15H15N. In a article£¬once mentioned of 118864-75-8

Diastereoselective addition of chiral (2-lithiophenyl)acetaldehyde acetals to various imines as key step in the asymmetric synthesis of 1- aryltetrahydroisoquinolines, part 4

A novel asymmetric synthesis of 1-aryl-1,2,3,4-tetrahydroisoquinolines has been developed. The key step in this synthesis is the diastereoselective addition of homochiral (2-lithiophenyl)acetaldehyde acetals to the sulfonylimine 25 and to the arylimines 28 and 31. The best diastereoselectivity is obtained by addition of the bis(2-methoxypropan-2- yl)-substituted 1,3-dioxolane 6e to benzylidene-p-anisidine (31) with an HPLC-determined diastereomeric ratio 32c/33c = 92.1:7.9. The N-tosyl and the N-(4-methoxyphenyl) groups of the addition products 26d, 27d, 32c, and 33c are cleaved with sodium in liquid ammonia and ammonium cerium(IV) nitrate, respectively, to yield the primary amines 35 and 36. The acid-catalysed cyclization of the sulfonamides 26d and 27d and the carbamates 37 and 38, prepared from 35 and 36, leads to the enantiomerically pure dihydroisoquinolines 40 and 41, respectively. During the cyclization of the sulfonamides 26d, 27d and the carbamates 37, 38 the chiral auxiliary – the diol 39 – is cleaved unchanged and can be recovered in good yields.

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

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, SDS of cas: 118864-75-8, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C15H15N

Enantioselective iridium-catalyzed hydrogenation of 1- and 3-substituted isoquinolinium salts

Asymmetric hydrogenation: The title reaction provides an efficient and rapid access to chiral 1- and 3-substituted 1,2,3,4-tetrahydroisoquinolines with excellent enantioselectivity (see scheme; L=ligand). A preliminary mechanistic study indicates that the 1,2-hydride addition might be the initial step in the reaction. The method has been used in the synthesis of urinary antispasmodic drug (+)-solifenacin. Copyright

Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. SDS of cas: 118864-75-8, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 118864-75-8, in my other articles.

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

Application of 118864-75-8, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.118864-75-8, Name is (S)-1-Phenyl-1,2,3,4-tetrahydroisoquinoline, molecular formula is C15H15N. In a Article£¬once mentioned of 118864-75-8

Bringing biocatalytic deuteration into the toolbox of asymmetric isotopic labelling techniques

Enzymes dependent on nicotinamide cofactors are important components of the expanding range of asymmetric synthetic techniques. New challenges in asymmetric catalysis are arising in the field of deuterium labelling, where compounds bearing deuterium (2H) atoms at chiral centres are becoming increasingly desirable targets for pharmaceutical and analytical chemists. However, utilisation of NADH-dependent enzymes for 2H-labelling is not straightforward, owing to difficulties in supplying a suitably isotopically-labelled cofactor ([4-2H]-NADH). Here we report on a strategy that combines a clean reductant (H2) with a cheap source of 2H-atoms (2H2O) to generate and recycle [4-2H]-NADH. By coupling [4-2H]-NADH-recycling to an array of C=O, C=N, and C=C bond reductases, we demonstrate asymmetric deuteration across a range of organic molecules under ambient conditions with near-perfect chemo-, stereo- and isotopic selectivity. We demonstrate the synthetic utility of the system by applying it in the isolation of the heavy drug (1S,3?R)-[2?,2?,3?-2H3]-solifenacin fumarate on a preparative scale.

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