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Process for the Preparation of Doxazosin and Salts Thereof

The present invention relates to a process for the preparation of doxazosin or salts thereof.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Containing 1,4-benzodioxane structure of the pyrazoline derivatives and the preparation and use thereof (by machine translation)

A the inflammation contains 1,4-benzodioxane structure of the pyrazoline derivatives, its characteristic is that it has the following formula: In the structural formula of R 1 to: R 2 to: R 3 to: […] derivatives of this invention can be used as a potential antibacterial and anti-tumor drug. The present invention discloses the preparation method. (by machine translation)

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis and alpha-blocking activity of some cyclic and opened analogues of WB 4101

The synthesis of some cyclic and open analogues of 2-(2,6-dimethoxyphenoxyethylaminomethyl)-1,4-benzodioxane (1, WB 4101) is described. The blocking activity of this compound and its analogues (1-5) was determined on the pre- and postsynaptic alpha-adrenoceptors of isolated rat vas deferens to investigate the structural requirements for conpetitive alpha-adrenoceptor occupancy by antagonists of the benzodioxane class. The activities of 1-5 at the presynaptic alpha-adrenoceptor were not significantly different whereas there were differences among the compounds of at least two orders of magnitude at the postsynaptic alpha-adrenoceptor. This clearly indicates that the structural requirements at the presynaptic receptor level are less restrictive than those required by the postsynaptic alpha-adrenoceptor. The symmetric analogues 3 and 4 were significantly weaker postsynaptic alpha-antagonists compared to 1. On the other hand, 2 and 5 displayed a very high postsynaptic activity, almost comparable to that of 1. These findings might suggest that the antagonists of the benzodioxane class do not bind at two identical aromatic sites symmetrically arranged around the anionic site of the alpha-adrenoceptor. Indeed, they might indicate that the benzodioxane binding site(s) incorporates two areas with very similar but not identical structural requirements. Furthermore, the very high activity of 5 may suggest that the benzodioxane nucleus is not essential to activity.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

Simple exploration of (S)-1,4-Benzodioxane-2-carboxylic acid

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Regio- and stereoselective Pd-catalyzed direct arylation of unactivated sp3 C(3)-H bonds of tetrahydrofuran and 1,4-benzodioxane systems

An auxiliary-enabled Pd-catalyzed highly regio- and stereoselective sp3 C-H activation and the direct arylation of the C3-position of oxygen heterocycles, such as tetrahydrofuran and 1,4-benzodioxane systems, are reported. An efficient stereoselective construction of cis 2,3-disubstituted tetrahydrofuran derivatives (analogues of norlignans) and cis 2,3-disubstituted 1,4-benzodioxane derivatives (analogues of neolignans) is described. The direct C(sp3)-H arylation of the C3-position of (R)- or (S)- tetrahydrofuran-2-carboxamides furnished the corresponding (2R,3R) and (2S,3S) C3-arylated THF scaffolds as major compounds with very high regio- and diastereoselectivities. The stereochemistry of the products obtained in this work were unambiguously assigned on the basis of the X-ray structure analyses of representative compounds 3b, 3e, 4p, and 7.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Discovery and development of the novel potent orally active thrombin inhibitor N-(9-hydroxy-9-fluorenecarboxy)prolyl trans-4-aminocyclohexylmethyl amide (L-372,460): Coapplication of structure-based design and rapid multiple analogue synthesis on solid support

Early studies in these laboratories of peptidomimetic structures containing a basic P1 moiety led to the highly potent and selective thrombin inhibitors 2 (K(i) = 5.0 nM) and 3 (K(i) = 0.1 nM). However, neither attains significant blood levels upon oral administration to rats and dogs. With the aim of improving pharmacokinetic properties via a more diverse database, we devised a resin-based route for the synthesis of analogues of these structures in which the P3 residue is replaced with a range of lipophilic carboxylic amides. Assembly proceeds from the common P2-P1 template 7 linked via an acid-labile carbamate to a polystyrene support. Application of the methodology in a repetitive fashion afforded several interesting analogues out of a collection of some 200 compounds. Among the most potent of the group, N-(9-hydroxy-9-fluorenecarboxy)-prolyl trans-4- aminocyclohexylmethyl amide (L-372,460 8, K(i) = 1.5 nM), in addition to being fully efficacious in a rat model of arterial thrombosis at an infusion rate of 10 mug/kg/min, exhibits oral bioavailability of 74% in dogs, and oral bioavailability of 39% in monkeys with a serum half-life of just under 4 h. On the basis of its favorable biological properties, inhibitor 8 has been subject to further evaluation as a possible treatment for thrombogenic disorders.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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HETEROARYL DISULFIDE COMPOUNDS AS ALLOSTERIC EFFECTORS FOR INCREASING THE OXYGEN-BINDING AFFINITY OF HEMOGLOBIN

This invention relates to compounds of Formula I: (Formula I), and pharmaceutically acceptable salt thereof, which are allosteric effectors that increase the oxygen-being affinity of hemoglobin, which are useful in the treatment of sickle cell disease, high altitude tissue hypoxia, and other conditions.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

More research is needed about (S)-1,4-Benzodioxane-2-carboxylic acid

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Decarboxylative Alkynylation and Carbonylative Alkynylation of Carboxylic Acids Enabled by Visible-Light Photoredox Catalysis

Visible-light-induced photocatalytic decarboxylative alkynylations of carboxylic acids have been developed for the first time. The reaction features extremely mild conditions, broad substrate scope, and avoids additional oxidants. Importantly, a decarboxylative carbonylative alkynylation has also been carried out in the presence of carbon monoxide (CO) under photocatalytic conditions, which affords valuable ynones in high yields at room temperature.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Selective alpha-Oxyamination and Hydroxylation of Aliphatic Amides

Compared to the alpha-functionalization of aldehydes, ketones, even esters, the direct alpha-modification of amides is still a challenge because of the low acidity of alpha-CH groups. The alpha-functionalization of N?H (primary and secondary) amides, containing both an unactived alpha-C?H bond and a competitively active N?H bond, remains elusive. Shown herein is the general and efficient oxidative alpha-oxyamination and hydroxylation of aliphatic amides including secondary N?H amides. This transition-metal-free chemistry with high chemoselectivity provides an efficient approach to alpha-hydroxy amides. This oxidative protocol significantly enables the selective functionalization of inert alpha-C?H bonds with the complete preservation of active N?H bond.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

New explortion of (S)-1,4-Benzodioxane-2-carboxylic acid

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Nickel-Catalyzed Reduction of Secondary and Tertiary Amides

The nickel-catalyzed reduction of secondary and tertiary amides to give amine products is reported. The transformation is tolerant of extensive variation with respect to the amide substrate, proceeds in the presence of esters and epimerizable stereocenters, and can be used to achieve the reduction of lactams. Moreover, this methodology provides a simple tactic for accessing medicinally relevant alpha-deuterated amines.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem

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Synthesis of diamides from 1,4-Benzodioxane-2-and isochroman-1-carboxylic acids

1,4-Benzodioxane-2-carboxylic acid and isochroman-1-carboxylic acid were treated with thionyl chloride, and the resulting acid chlorides reacted with p-aminobenzoic acid in dioxane in the presence of pyridine to produce the corresponding amido acids. The latter were converted into acid chlorides which were brought into reaction with various amines to obtain a number of new diamides.

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Benzodioxan,
1,4-Benzodioxane | C8H8O2 – PubChem