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One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide

A process for the preparation of 1,2-benzisoxazole-3-methane-sulfonamide without isolation of intermediates in solid form, by using 4-hydroxycoumarin as a starting compound, and water and 1,2-dichloro-ethane as solvents; and an industrially useful process for the preparation of 1,2-benzisoxazole-3-acetic acid, by reacting 4-hydroxycoumarin and hydroxylamine in water.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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DOES CHLORINATION MODIFY THE AUXIN-LIKE ACTIVITY OF 1,2-BENZISOXAZOLE-3-ACETIC ACID?

The insertion of a chlorine atom in different positions of the aromatic ring did not increase the activity of benzisoxazole acetic acid, a new synthetic growth regulator, on shoot regeneration in vitro, pea stem elongation or flax root growth.This shows that this compound behaves differently from other synthetic auxins, and suggests that its activity is mainly related to the structure of its ring.Key Word Index – Chlorinated benzisoxazolic acetic acid; auxin-like activities; in vitro shoot regeneration; pea stem elongation; flax root growth.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. Application In Synthesis of 1,2-Benzisoxazole-3-acetic Acid, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 4865-84-3, name is 1,2-Benzisoxazole-3-acetic Acid. In an article£¬Which mentioned a new discovery about 4865-84-3

1,2-Benzisoxazole Phosphorodiamidates as Novel Anticancer Prodrugs Requiring Bioreductive Activation

Several 1,2-benzisoxazole phosphorodiamidates have been designed as prodrugs of phosphoramide mustard requiring bioreductive activation. Enzymatic reduction of 1,2-benziosoxazole moiety is expected to result in the formation of imine intermediate due to the cleavage of the N-O bond. The imine should then be spontaneously hydrolyzed to a ketone metabolite, thereby facilitating base-catalyzed beta-elimination of cytotoxic phosphoramide mustard. As expected, the proposed prodrugs 4, 9, and 12 were at least 3-5-fold more potent cytotoxins than control compounds 5 and 15, which lack in the phosphoramide mustard group. Upon incubation with phenobarb-induced rat liver S-9 fraction, compounds 4, 9, and 12 underwent extensive NADPH-dependent metabolism with concomitant generation of alkylating activity under both hypoxic and oxic conditions. Corresponding ketone metabolites were detected for 9 and 15. NADPH-dependent bioreduction of 15 to its ketone metabolite 16 was located in the microsomal fraction and inhibited by SKF-525A and pCMBA. Compared with phenobarb-induced rat liver microsomal fraction, incubation of 15 with rat or human P450 reductase microsomes showed moderate generation of 16. Microsomal cytochrome P450 and/or P450 reductase appear to be involved in the reductive metabolism of 1,2-benzisoxazole moiety under hypoxic as well as oxic conditions.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Facile preparation of protected benzylic and heteroarylmethyl amines via room temperature Curtius rearrangement

A step-wise, room temperature procedure for acyl azide formation and the subsequent Curtius rearrangement of phenyl and heteroaryl acetic acids is described. We have developed a protocol for room temperature Curtius rearrangement in MeOH or CHCl3 that provides an improvement over standard conditions, avoiding the use of additives or heat. This room temperature optimization of the Curtius rearrangement prevents the formation of side products often observed with benzylic acids, allowing access to a variety of benzylic and heteroarylmethyl amines.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide

A process for the preparation of 1,2-benzisoxazole-3-methane-sulfonamide without isolation of intermediates in solid form, by using 4-hydroxycoumarin as a starting compound, and water and 1,2-dichloro-ethane as solvents; and an industrially useful process for the preparation of 1,2-benzisoxazole-3-acetic acid, by reacting 4-hydroxycoumarin and hydroxylamine in water.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS

The present invention relates to phenyl-substituted heterocyclyl derivatives of the formula (I) wherein Z, n, m, R1, R2, R3, R4, R5, R6, R7 and R8 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Piperidine derivatives having anxiolytic effect

Piperidine compounds having the general formula (I), STR1 wherein R 1 is a group having general formula (II), STR2 wherein X is CHR 10, O, S, SO, SO 2 or NR 10, Z 1 is CH 2, O, or S; Z 2 and Z 3 are independently (CH 2) n, n being 0 or 1, O or S or Z 1 and Z 2 may together represent a group –CH CH–; or when Z 3 is (CH 2) n wherein n is 0, Z 1 and Z 2 may together represent a 3-membered divalent group; show potent sigma receptor activity. Furthermore they show effect in animal models indicative of anxiolytic properties. Accordingly they are useful as medicines for the treatment of anxiety, psychosis, epilepsy, convulsion, movement disorders, motor disturbances, amnesia, cerebrovascular diseases, senile demential of the Alzheimer type or Parkinson”s disease.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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NEW SOMATOSTATIN RECEPTOR SUBTYPE 4 (SSTR4) AGONISTS

The invention relates to 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Discovery of 1,2-Benzisoxazole-3-acetic Acid

Because enzymes can increase reaction rates by enormous factors and tend to be very specific, Computed Properties of C9H7NO3, typically producing only a single product in quantitative yield, they are the focus of active research.you can also check out more blogs about Computed Properties of C9H7NO3

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METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION

The present invention relates to compositions of minoxidil and Sonic Hedgehog (Shh) pathway activators and optionally, Wnt agonists and methods of using them to induce self-renewal of hair follicle stem cells, including inducing the hair follicle stem cells to proliferate while maintaining, in the daughter cells, the capacity to differentiate into hair follicle epithelial cells.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Optimization of Potent ATAD2 and CECR2 Bromodomain Inhibitors with an Atypical Binding Mode

Most bromodomain inhibitors mimic the interactions of the natural acetylated lysine (KAc) histone substrate through key interactions with conserved asparagine and tyrosine residues within the binding pocket. Herein we report the optimization of a series of phenyl sulfonamides that exhibit a novel mode of binding to non-bromodomain and extra terminal domain (non-BET) bromodomains through displacement of a normally conserved network of four water molecules. Starting from an initial hit molecule, we report its divergent optimization toward the ATPase family AAA domain containing 2 (ATAD2) and cat eye syndrome chromosome region, candidate 2 (CECR2) domains. This work concludes with the identification of (R)-55 (GSK232), a highly selective, cellularly penetrant CECR2 inhibitor with excellent physicochemical properties.

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Reference£º
Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics