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Synthetic Route of 214894-89-0, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

The invention relates to a radioisotope-labelled compound of quaternary ammonium salt of a polycyclic aromatic amine with formula I, wherein the wavy line indicates a single bond between the non-nodal carbon atom of a polycyclic aromatic system and the R1 substituent. In formula I, R1 substituent is independently selected from hydrogen, halogens, a hydroxy optionally protected, C1-4alkoxy, a nitro group, an amino group optionally having 1 or 2 hydrogen atoms replaced with C1-6alkyl or having 2 atoms of hydrogen replaced with C2-5alkylene to form a heterocyclic ring, a chain C1-6carbon group optionally having a halogen, carboxy, formyl or C1-4alkanesulfonic substituent, and a phenyl group optionally having 1-5 substituents independently selected from halogens, a chain C1-6carbon, a halogenated chain Cl-6carbon substituent, a hydroxy optionally protected, C1-4alkoxy, an amino group optionally having 1-2 atoms of hydrogen replaced with C1-6alkyl; R2 is a chain aliphatic substituent having the-CH2- fragment as the terminal member of the chain, to which chain a phenyl group is optionally attached optionally having 1-3 substituents selected from halogens and C1-6alkyl, and, if the chain contains at least 2 carbon atoms, in which chain there is optionally a bivalent link between the carbon atoms, said link selected from the oxygen atom -O-, sulfur atom -S- and C3-6cycloalkylene, wherein the R2 substituent contains a total of 1-16 carbon atoms, and the hydrogen atom at one of the carbon atoms is replaced with an atom of 18F fluorine radioisotope; R3 and R4 are combined to form a bivalent butadienyl-1,3 substituent whose terminal carbon atoms are linked to the adjacent non-nodal carbon atoms of the B ring to form an aromatic C ring fused with the A and B ring system having R1 substituents at non-nodal carbon atoms; n is an integer of 9; X- is a pharmaceutically acceptable counterion, which is an anion of a mono-basic inorganic acid, a mononegative anion of a multi-basic inorganic acid, an anion of an alkanecarboxylic acid, an anion of an aliphatic sulfonic acid, an anion of an aromatic sulfonic acid, an anion of an acidic amino acid; as well as a hydrate or solvate thereof. The invention also relates to the use of the compound according to the invention and a pharmaceutical composition comprising the compound according to the invention.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reference of 214894-89-0, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine. In a Patent, once mentioned of 214894-89-0.

This disclosure relates to compounds that inhibit histone demethylase activity. In particular, the disclosure relates to compounds that inhibit histone lysine demethylase KDM5B, pharmaceutical compositions and methods of use, such as methods of treating cancer using the compounds and pharmaceutical compositions disclosed herein.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reference of 214894-89-0, New Advances in Chemical Research, May 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. In a document type is Patent, and a compound is mentioned, 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, introducing its new discovery.

The present invention relates to compound of Formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with RNA-viruses belonging to the family of the Retroviridae, the family of the Flaviviridae and the family of the Picornaviridae and more preferably infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent viral infections. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of viral disorders and pathologic conditions such as, but not limited to, viral infections with Human Immunodeficiency Virus 1 (HIV1), Human Immunodeficiency Virus 2 (HIV2), Hepatitis C virus (HCV), Dengue virus, and enteroviruses like Coxsackievirus, Rhinovirus and Poliovirus.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Reference of 214894-89-0, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

A series of novel, highly potent, achiral factor Xa inhibitors based on a benzoic acid scaffold and containing a chlorophenethyl moiety directed towards the protease S1 pocket is described. A number of structural features, such as the requirements of the P1, P4 and ester-binding pocket ligands were explored with respect to inhibition of factor Xa. Compound 46 was found to be the most potent compound in a series of antithrombotic secondary assays.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Oleuropein is a glucosylated seco-iridoid present in olive fruits and leaves. Due to its broad spectrum of biological activities, including anticancer properties, oleuropein has attracted scientific attention for the past 20 years. The promising antiproliferative activity of an olive leaf extract enriched in oleuropein against a series of human cancer cell lines, prompted us to proceed with the semi-synthesis of 51 analogs of oleuropein. Following their initial screening against the estrogen receptor negative breast cancer cell line SKBR3, 7 analogs were shown to display significant cytotoxicity and were further tested against 6 additional solid tumor-derived and leukemic cell lines. The analog with the most promising antitumor activity (24) was selected for more detailed studies. 24 was non-toxic to peripheral blood mononuclear cells derived from healthy blood donors when tested at concentrations close to its half maximal inhibitory concentration. In vivo administration of 24 in melanoma-bearing mice resulted in reducing tumor size in a dose-dependent manner and in inducing anti-melanoma-reactive immune responses. Our results suggest that analog 24, emerging from the initial structure of oleuropein, represents a promising lead structure for further optimization.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Related Products of 214894-89-0, Chemical Research Letters, May 2021. The appropriate choice of redox mediator can avoid electrode passivation and overpotential, which strongly inhibit the efficient activation of substrates in electrolysis. 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine,introducing its new discovery.

Treatment of baker’s yeast with phenacyl chloride in an aqueous-organic solvent has been proven to be an effective method of inhibiting the enzymes that afford (S)-enantiomers of alpha-hydroxy esters in the reduction of alpha-keto esters. The procedure is effective for the whole-cell system to produce the (R)-product with high chemical yield and high enantiomeric excess.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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We report a one-step, Ru(II)-catalyzed cyclopropanation reaction that is conceptually different from the previously reported protocols that include Corey-Chaykovsky, Simmons-Smith, and metal-catalyzed carbene attack on olefins. Under the current protocol, various alcohols and esters are transformed into sulfone substituted cyclopropanes with excellent isolated yields and diastereoselectivities. This new reaction forms highly congested cyclopropane products with three new C-C bonds, three or two new chiral centers and one new quaternary carbon center. Twenty-two examples of isolated substrates are given. Previously reported synthetic routes for similar substrates are all multistep, linear routes that proceed with overall low yields and poor control of stereochemistry. Commercially available Ru(II) dehydrogenation catalysts, that were recently developed for the dehydrogenative synthesis of esters and amides from alcohol and amine substrates, were used in the reaction, with the best catalyst showing excellent activity at 0.2-1 mol % catalyst loading. Mechanistic investigation showed that in the case of alcohol substrates, the catalyst is only responsible for the first dehydrogenation step, and that the identity of the base and the countercation is crucial in achieving high yields. The catalyst is also required for the cyclopropanation of esters, although no dehydrogenation can proceed in this case, suggesting that substrates sensitive to H2 may be acylated prior to reaction.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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We’ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 214894-89-0, and how the biochemistry of the body works.COA of Formula: C9H9BrO2

Research speed reading in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic. Recommanded Product: 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, In a article, mentioned the application of 214894-89-0, Name is 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine, molecular formula is C9H9BrO2

A series of 4-substituted phenoxypropanolamines was prepared and examined for beta-adrenoceptor activity.Some of the compounds, especially the <4-<2-<<2-(4-fluorophenyl)ethyl>oxy>ethoxy>phenoxy>propanolamines (14, 15, and 24), showed potent beta1-blockade with virtually no beta2-blockade at doses over a 1000 times greater.The compounds also possessed partial agonist activity.Structure-activity relationships are discussed, and conclusions are drawn about the binding sites on beta-adrenoceptors.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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We report the preliminary results of the synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a number of phenyl alkyl imidazole-based compounds as inhibitors of the two components of 17alpha-hydroxylase/17,20-lyase (P45017alpha), that is, 17alpha-hydroxylase (17alpha-OHase) and 17,20-lyase (lyase). The results show that N-3-(4-bromophenyl) propyl imidazole (12) (IC50 = 2.95 muM against 17alpha-OHase and IC50 = 0.33 muM against lyase) is the most potent compound within the current study, in comparison to ketoconazole (KTZ) (IC50 = 3.76 muM against 17alpha-OHase and IC50 = 1.66 muM against lyase). Modelling of these compounds suggests that the length of the alkyl chain enhances the interaction between the inhibitor and the area of the active site corresponding to the C(3) area of the steroid backbone, thereby increasing potency.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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In this paper we describe the synthesis of a series of alpha-substituted analogues of the potent and selective group II metabotropic glutamate receptor (mGluR) agonist (1S,1’S,2’S)-carboxycyclopropylglycine (2, L-CCG 1). Incorporation of a substituent on the amino acid carbon converted the agonist 2 into an antagonist. All of the compounds were prepared and tested as a series of four isomers, i.e., two racemic diastereomers. On the basis of the improvement in affinity realized for the alpha-phenylethyl analogue 3, in this paper we explored the effects of substitution on the aromatic ring as a strategy to increase the affinity of these compounds for group II mGluRs. Affinity for group II mGluRs was measured using [3H]glutamic acid (Glu) binding in rat forebrain membranes. Antagonist activity was confirmed for these compounds by measuring their ability to antagonize (1S,3R)-1- aminocyclopentane-1,3-dicarboxylic acid-induced inhibition of forskolin stimulated cyclic-AMP in RGT cells transfected with human mGluR2 and mGluR3. Meta substitution on the aromatic ring of 3 with a variety of substituents, both electron donating (e.g., methyl, hydroxy, amino, methoxy, phenyl, phenoxy) and electron withdrawing (e.g., fluorine, chlorine, bromine, carboxy, trifluoromethyl) gave from 1.5- to 4.5-fold increases in affinity. Substitution with p-fluorine, as in 97 (IC50 = 0.022 ± 0.002), was the exception. Here, a greater increase in affinity was realized than for either the ortho- or meta-substituted analogues; 97 was the most potent compound resulting from monosubstitution of the aromatic. At best, only modest increases in affinity were realized for certain compounds bearing either two chlorines or two fluorines, and two methoxy groups gave no improvement in affinity (all examined in a variety of substitution patterns). Three amino acids, 4, 5, and 104, were resolved into their four constituent isomers, and affinity and functional activity for group II mGluRs was found to reside solely in the S,S,S-isomers of each, consistent with 1. With an IC50 = 2.9 ± 0.6 nM, the resolved xanthylmethyl compound 168 was the most potent compound from this SAR. Amino acid 168 demonstrated high plasma levels following intraperitoneal (ip) administration and readily penetrated into the brain. This compound, however, had only limited (~5%) oral bioavailability. Systemic administration of 168 protected mice from limbic seizures produced by the mGluR agonist 3,5-dihydroxyphenylglycine, with an ED50 = 31 mg/kg (ip, 60 min preinjection). Thus, 168 represents a valuable tool to study the role of group II mGluRs in disease.

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Reference:
Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem