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SUBSTITUTED PHENOXY-AMINOPROPANOLS

Substituted phenoxy-aminopropanols of the formula STR1 wherein R is a branched-chain alkyl of 3 or 4 carbon atoms, R 1 is hydrogen, halogen or lower alkyl and R 2 and R 3, independently, are hydrogen, halogen, lower alkyl, lower alkoxy or lower alkylthio, and pharmaceutically acceptable acid addition salts thereof, are described. A process for their preparation, as well as pharmaceutical preparations containing them are also described. The compounds of formula I and their salts possess cardioselective beta-adrenergic blocking activity and antihypertensive activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

The important role of 5-(Bromomethyl)-2,3-dihydro-1,4-benzodioxine

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Kinetics and Mechanism of the Arase-Hoshi R2BH-Catalyzed Alkyne Hydroboration: Alkenylboronate Generation via B-H/C-B Metathesis

The mechanism of R2BH-catalyzed hydroboration of alkynes by 1,3,2-dioxaborolanes has been investigated by in situ 19F NMR spectroscopy, kinetic simulation, isotope entrainment, single-turnover labeling (10B/2H), and density functional theory (DFT) calculations. For the Cy2BH-catalyzed hydroboration 4-fluorophenylacetylene by pinacolborane, the resting state is the anti-Markovnikov addition product ArCH = CHBCy2. Irreversible and turnover-rate limiting reaction with pinacolborane (k ? 7 ¡Á 10-3 M-1 s-1) regenerates Cy2BH and releases E-Ar-CH?CHBpin. Two irreversible events proceed in concert with turnover. The first is a Markovnikov hydroboration leading to regioisomeric Ar-C(Bpin)?CH2. This is unreactive to pinacolborane at ambient temperature, resulting in catalyst inhibition every ?102 turnovers. The second is hydroboration of the alkenylboronate to give ArCH2CH(BCy2)Bpin, again leading to catalyst inhibition. 9-BBN behaves analogously to Cy2BH, but with higher anti-Markovnikov selectivity, a lower barrier to secondary hydroboration, and overall lower efficiency. The key process for turnover is B-H/C-B metathesis, proceeding by stereospecific transfer of the E-alkenyl group within a transient, mu-B-H-B bridged, 2-electron-3-center bonded B-C-B intermediate.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Iron-Catalyzed Borrowing Hydrogen beta- C(sp3)-Methylation of Alcohols

Herein we report the iron-catalyzed beta-C(sp3)-methylation of primary alcohols using methanol as a C1 building block. This borrowing hydrogen approach employs a well-defined bench-stable (cyclopentadienone)iron(0) carbonyl complex as precatalyst (5 mol %) and enables a diverse selection of substituted 2-arylethanols to undergo beta-C(sp3)-methylation in good isolated yields (24 examples, 65% average yield).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis and immunosuppressant activity of pyrazole carboxamides

A series of novel pyrazole carboxamides sis disclosed that demonstrate strong immunosuppressant activity in rodent and human mixed leukocyte response (MLR) assays (IC50 < 1 muM). The synthesis, biological activity, mode of action, and pharmacokinetic properties of this new lead series are discussed. Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.SDS of cas: 214894-89-0, you can also check out more blogs about214894-89-0

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Direct C-OH/P(O)-H dehydration coupling forming phosphine oxides

A t-BuONa-mediated C-OH/P(O)-H cross dehydration coupling to produce alkylphosphine oxides is developed. This reaction employed readily available alcohols and P(O)-H compounds as the starting materials, providing an efficient alternative method for constructing sp3 C-P bonds. A reasonable reaction path involving dehydration and subsequent regio-selective hydrophosphorylation of the resulting alkenes was proposed.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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FUNGAL HYDROXYLATION OF ETHYL BENZENE AND DERIVATIVES

The fungus Mortierella isabellina converts ethyl benzene and a number of para-substituted derivatives to the corresponding optically active 1-phenylethanols with enantiomeric excesses between 5 and 40percent.Hydrogen removal from the substrate preceeds product formation and is stereochemically independent of it.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Functionalization at position 3 of the phenyl ring of the potent mGluR5 noncompetitive antagonists MPEP

We described the synthesis and biological evaluation of MPEP analogs functionalized at the position 3 of the phenyl ring. The results point out the limitation in the choice of a functional group at this position; the only substituents leading to retention of activity are NO2 (IC 50 = 13 nM) and CN (IC50 = 8 nM).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Cascade bio-hydroxylation and dehalogenation for one-pot enantioselective synthesis of optically active beta-halohydrins from halohydrocarbons

A stereoselective hydroxylation and enantioselective dehalogenation cascade reaction was developed for the synthesis of optically active beta-haloalcohols from halohydrocarbons. This cascade system employed P450 and halohydrin dehalogenase as two compatible biocatalysts, allowing a straightforward, greener and efficient access to beta-halohydrins with excellent enantioselectivities (98-99%).

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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2-ALKYL-INDAZOLE COMPOUNDS FOR THE TREATMENT OF CERTAIN CNS-RELATED DISORDERS

2-Alkyl-indazole compound and its pharmaceutically acceptable salts of acid addition, method and intermediates for preparing them, a pharmaceutical composition containing them and use of the latter. The 2-alkyl-indazole compound has the following general formula (I) in which R1, R2, R3, R4, R6, R7, X, Y, W, n, p, and m have the meanings stated in the description.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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SELECTIVE INHIBITORS OF NLRP3 INFLAMMASOME

The present disclosure relates to compounds of Formula (I): (I); and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein are useful for inhibiting the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as autoinflammatory and autoimmune diseases and cancers.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem