Category: 42923-79-5

One of the major reasons for studying chemical kinetics is to use measurements of the macroscopic properties of a system, Application In Synthesis of 7-Nitro-1,2,3,4-tetrahydroisoquinoline, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 42923-79-5, Name is 7-Nitro-1,2,3,4-tetrahydroisoquinoline, molecular formula is C9H10N2O2

Dehydrogenation of Nitrogen Heterocycles Using Graphene Oxide as a Versatile Metal-Free Catalyst under Air

Graphene oxide (GO) has been developed as an inexpensive, environmental friendly, metal-free carbocatalyst for the dehydrogenation of nitrogen heterocycles. Valuable compounds, such as quinoline, 3,4-dihydroisoquinoline, quinazoline, and indole derivatives, have been successfully used as substrates. The investigation of various oxygen-containing molecules with different conjugated systems indicated that both the oxygen-containing groups and large pi-conjugated system in GO sheets are essential for this reaction. (Figure presented.).

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

In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Formula: C9H10N2O2, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 42923-79-5, name is 7-Nitro-1,2,3,4-tetrahydroisoquinoline. In an article£¬Which mentioned a new discovery about 42923-79-5

3-(3,4-dihydroisoquinolin-2(1 H)-ylsulfonyl)benzoic acids: Highly potent and selective inhibitors of the type 5 17-beta-hydroxysteroid dehydrogenase AKR1C3

A high-throughput screen identified 3-(3,4-dihydroisoquinolin-2(1H)- ylsulfonyl)benzoic acid as a novel, highly potent (low nM), and isoform-selective (1500-fold) inhibitor of aldo-keto reductase AKR1C3: a target of interest in both breast and prostate cancer. Crystal structure studies showed that the carboxylate group occupies the oxyanion hole in the enzyme, while the sulfonamide provides the correct twist to allow the dihydroisoquinoline to bind in an adjacent hydrophobic pocket. SAR studies around this lead showed that the positioning of the carboxylate was critical, although it could be substituted by acid isosteres and amides. Small substituents on the dihydroisoquinoline gave improvements in potency. A set of “reverse sulfonamides” showed a 12-fold preference for the R stereoisomer. The compounds showed good cellular potency, as measured by inhibition of AKR1C3 metabolism of a known dinitrobenzamide substrate, with a broad rank order between enzymic and cellular activity, but amide analogues were more effective than predicted by the cellular assay.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to 42923-79-5, help many people in the next few years.Formula: C9H10N2O2

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

Chemistry is traditionally divided into organic and inorganic chemistry. Application In Synthesis of 7-Nitro-1,2,3,4-tetrahydroisoquinoline, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 42923-79-5

Electron-donating para-methoxy converts a benzamide-isoquinoline derivative into a highly Sigma-2 receptor selective ligand

The sigma-2 (sigma2) receptor has been suggested to be a promising target for pharmacological interventions to curb tumor progression. Development of sigma2-specific ligands, however, has been hindered by lack of understanding of molecular determinants that underlie selective ligand-sigma2 interactions. Here we have explored effects of electron donating and withdrawing groups on ligand selectivity for the sigma2 versus sigma1 receptor using new benzamide-isoquinoline derivatives. The electron-donating methoxy group increased but the electron-withdrawing nitro group decreased sigma2 affinity. In particular, an extra methoxy added to the para-position (5e) of the benzamide phenyl ring of 5f dramatically improved (631 fold) the sigma2 selectivity relative to the sigma1 receptor. This para-position provided a sensitive site for effective manipulation of the sigma receptor subtype selectivity using either the methoxy or nitro substituent. Our study provides a useful guide for further improving the sigma2-over-sigma1 selectivity of new ligands.

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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, 42923-79-5, name is 7-Nitro-1,2,3,4-tetrahydroisoquinoline, introducing its new discovery. name: 7-Nitro-1,2,3,4-tetrahydroisoquinoline

HETEROCYCLIC CYCLOPENTYL TETRAHYDROISOQUINOLINE AND TETRAHYDROPYRIDOPYRIDINE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The present invention is directed to compounds of formula (I), wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, X, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.

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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, HPLC of Formula: C9H10N2O2, such as the rate of change in the concentration of reactants or products with time.In a article, mentioned the application of 42923-79-5, Name is 7-Nitro-1,2,3,4-tetrahydroisoquinoline, molecular formula is C9H10N2O2

A cobalt catalytic hydroformylation reaction synthesis carboxamide derivatives (by machine translation)

The invention discloses a cobalt catalytic hydroformylation reaction synthesis carboxamide derivatives of the method, the method is that the amine compound with the formyl compound in the cobalt salt under the catalytic action of a one-pot reaction to produce the carboxamide derivatives; the reaction of raw materials and catalyst are cheap and easily obtained, and the reaction step and the operation is simple, with high selectivity, high yield, can be expands the quantity reaction and the like, and overcomes the reaction reagent toxicity in the prior art large, expensive catalyst, more reaction steps, more byproducts and the like. (by machine translation)

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

42923-79-5, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 42923-79-5, C9H10N2O2. A document type is Article, introducing its new discovery.

Application of the goldilocks effect to the design of potent and selective inhibitors of phenylethanolamine N-methyltransferase: Balancing pKa and steric effects in the optimization of 3-methyl-1,2,3,4- tetrahydroisoquinoline inhibitors by beta-fluorination

3-Methyl-1,2,3,4-tetrahydroisoquinolines (3-methyl-THIQs) are potent inhibitors of phenylethanolamine N-methyltransferase (PNMT), but are not selective due to significant affinity for the alpha2-adrenoceptor. Fluorination of the methyl group lowers the pKa of the THIQ amine from 9.53 (CH3) to 7.88 (CH2F), 6.42 (CHF2), and 4.88 (CF3). This decrease in pKa results in a reduction in affinity for the alpha2-adrenoceptor. However, increased fluorination also results in a reduction in PNMT inhibitory potency, apparently due to steric and electrostatic factors. Biochemical evaluation of a series of 3-fluoromethyl-THIQs and 3-trifluoromethyl-THIQs showed that the former were highly potent inhibitors of PNMT, but were often nonselective due to significant affinity for the alpha2-adrenoceptor, while the latter were devoid of alpha2-adrenoceptor affinity, but also lost potency at PNMT. 3-Difluoromethyl-7-substituted-THIQs have the proper balance of both steric and pKa properties and thus have enhanced selectivity versus the corresponding 3-fluoromethyl-7-substituted-THIQs and enhanced PNMT inhibitory potency versus the corresponding 3-trifluoromethyl-7-substituted- THIQs. Using the “Goldilocks Effect” analogy, the 3-fluoromethyl-THIQs are too potent (too hot) at the alpha2-adrenoceptor and the 3-trifluoromethyl-THIQs are not potent enough (too cold) at PNMT, but the 3-difluoromethyl-THIQs are just right. They are both potent inhibitors of PNMT and highly selective due to low affinity for the alpha2- adrenoceptor. This seems to be the first successful use of the beta-fluorination of aliphatic amines to impart selectivity to a pharmacological agent while maintaining potency at the site of interest.

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

Chemistry is traditionally divided into organic and inorganic chemistry. 42923-79-5, The former is the study of compounds containing at least one carbon-hydrogen bonds.In a patent£¬Which mentioned a new discovery about 42923-79-5

COMPOUNDS AND METHODS

Disclosed are compounds having the formula (I): wherein R1, R2, R3, R4, R5, and R6 are as defined herein, and methods of making and using the same.

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

42923-79-5, Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 42923-79-5, C9H10N2O2. A document type is Article, introducing its new discovery.

Effects of a 3-alkyl-, 4-hydroxy- and/or 8-aromatic-substituent on the phenylethanolamine N-methyltransferase inhibitor potency and alpha2-adrenoceptor affinity of 2,3,4,5-tetrahydro-1H-2-benzazepines

2,3,4,5-Tetrahydro-1H-2-benzazepine (THBA; 1) is nearly 100-fold more selective an inhibitor of phenylethanolamine N-methyltransferase (PNMT, EC 2.1.1.28) versus the alpha2-adrenoceptor than is 1,2,3,4-tetrahydroisoquinoline (THIQ; 2) (1: PNMT Ki = 3.3 muM, alpha2-adrenoceptor Ki = 11 muM, selectivity [alpha2 Ki/PNMT Ki] = 3.3; 2: PNMT Ki = 9.7 muM, alpha2 Ki = 0.35 muM, selectivity = 0.036;). Since the PNMT inhibitory activity and selectivity of THIQ were enhanced by the introduction of a hydrophilic electron-withdrawing 7-substituent and a 3-alkyl-substituent, a similar study was conducted on THBA. 8-Nitro-THBA (3) was found to be as potent an inhibitor of PNMT as its THIQ analogue (21) and to be more selective due to its reduced alpha2-adrenoceptor affinity (3: PNMT Ki = 0.39 muM, alpha2 Ki = 66 muM, selectivity = 170; 21: PNMT Ki = 0.41 muM, alpha2 Ki = 4.3 muM, selectivity = 10). Introduction of a 3-alkyl substituent on the THBA nucleus decreased both the alpha2-adrenoceptor affinity and the PNMT inhibitory activity, suggesting an area of steric bulk intolerance at both sites. 4-Hydroxy-THBA (15), which can be considered a conformationally-restricted analogue of 3-hydroxymethyl-THIQ (30), exhibited poorer PNMT inhibitory activity and less selectivity than 30 (15: PNMT Ki = 58 muM, alpha2 Ki = 100 muM, selectivity = 1.7; 30: PNMT Ki = 1.1 muM, alpha2 Ki = 6.6 muM, selectivity = 6.0). While the addition of an 8-nitro group to 15 increased the selectivity of 16 as compared to its THIQ analogue (31), it was not as potent at PNMT nor as selective as 8-nitro-THBA (3) (16, PNMT Ki = 5.3 muM, alpha2 Ki = 680 muM, selectivity = 130; 31: PNMT Ki = 0.29 muM, alpha2 Ki = 19 muM, selectivity = 66). Compound 3 is the most selective (PNMT/alpha2) and one of the more potent at PNMT compounds yet reported in the benzazepine series, and should have sufficient lipophilicity to penetrate the blood-brain barrier (CLogP = 1.8).

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

Children learn through play, and they learn more than adults might expect. Science experiments are a great way to spark their curiosity, get their minds active, and encourage them to do something that doesn¡¯t involve a screen. 42923-79-5, C9H10N2O2. A document type is Article, introducing its new discovery., 42923-79-5

Tricyclic [1,2,4]triazine 1,4-dioxides as hypoxia selective cytotoxins

A series of novel tricyclic triazine-di-N-oxides (TTOs) related to tirapazamine have been designed and prepared. A wide range of structural arrangements with cycloalkyl, oxygen-, and nitrogen-containing saturated rings fused to the triazine core, coupled with various side chains linked to either hemisphere, resulted in TTO analogues that displayed hypoxia-selective cytotoxicity in vitro. Optimal rates of hypoxic metabolism and tissue diffusion coefficients were achieved with fused cycloalkyl rings in combination with both the 3-aminoalkyl or 3-alkyl substituents linked to weakly basic soluble amines. The selection was further refined using pharmacokinetic/pharmacodynamic model predictions of the in vivo hypoxic potency (AUCreq) and selectivity (HCD) with 12 TTO analogues predicted to be active in vivo, subject to the achievement of adequate plasma pharmacokinetics.

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

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.42923-79-5,7-Nitro-1,2,3,4-tetrahydroisoquinoline,as a common compound, the synthetic route is as follows.,42923-79-5

Into a 25 mL round-bottom flask was placed a solution of 7-nitro-1,2,3,4-tetrahydroisoquinoline (200 mg, 1.12 mmol) in dichloromethane (10 mL) followed by di-tert-butyl dicarbonate (489 mg, 2.24 mmol) and triethylamine (339 mg, 3.35 mmol). The reaction mixture was stirred overnight at room temperature then concentrated under vacuum. The residue was purified by column chromatography eluting with ethyl acetate/petroleum ether (1 :10). The collected fractions were combined and concentrated under vacuum to yield tert-butyl 7-nitro-3,4-dihydroisoquinoline-2(1H)-carboxylate (290 mg, 93%).

42923-79-5 7-Nitro-1,2,3,4-tetrahydroisoquinoline 6424833, atetrahydroisoquinoline compound, is more and more widely used in various fields.

Reference£º
Patent; LYCERA CORPORATION; AICHER, Thomas Daniel; SKALITZKY, Donald J.; TOOGOOD, Peter L.; VANHUIS, Chad A.; (416 pag.)WO2019/200120; (2019); A1;,
Tetrahydroisoquinoline – Wikipedia
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem