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Novel Base-induced Reactions of Substituted (1,2-Benzisoxazol-3-yl)acetates

The reactions of substituted (1,2-benzisoxazol-3-yl)acetates with strong bases are described.The esters (1) and (2) having electron-donating and dialkylamino substituents undergo novel ring transformations on treatment with NaH, ButOK, or MeONa in DMF to afford the 2H-azirines (8) and the 3-iminobenzofurans (18), respectively, while under similar conditions the halogeno esters (3) dimerize to give the ethylenedicarboxylate (24).Treatment of the esters (4)-(7) having electron-withdrawing substituents with NaH in DMF results in the recovery of the starting esters.However, on treatment of the sulphinyl esters (6) with MeONa in methanol, C-S bond cleavage occurs to afford methyl arylsulphinates (27).

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

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New Somatostatin receptor subtype 4 (SSTR4) agonists

3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.

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

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NEW OXABISPIDINE COMPOUNDS FOR THE TREATMENT OF CARDIAC ARRHYTHMIAS

There is provided compounds of formula I, [Chemical formula should be inserted here. Please see paper copy] wherein R1 to R4 , R41 to R46 and Z have meanings given in the description, which are useful in the prophylaxis and in the treatment of arrhythmias, in particular atrial and ventricular arrhythmias

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

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Structurally Diverse Mitochondrial Branched Chain Aminotransferase (BCATm) Leads with Varying Binding Modes Identified by Fragment Screening

Inhibitors of mitochondrial branched chain aminotransferase (BCATm), identified using fragment screening, are described. This was carried out using a combination of STD-NMR, thermal melt (Tm), and biochemical assays to identify compounds that bound to BCATm, which were subsequently progressed to X-ray crystallography, where a number of exemplars showed significant diversity in their binding modes. The hits identified were supplemented by searching and screening of additional analogues, which enabled the gathering of further X-ray data where the original hits had not produced liganded structures. The fragment hits were optimized using structure-based design, with some transfer of information between series, which enabled the identification of ligand efficient lead molecules with micromolar levels of inhibition, cellular activity, and good solubility.

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Benzisoxazole – Wikipedia,
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ARYL SUBSTITUTED OLEFINIC COMPOUNDS AS PDE10A INHIBITORS

The present invention provicles aryl substituted olefinic compounds as Phosphodiesterase 10A (PDE 10A) in- hibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders by inhibiting Phosphodiesterase 10A enzyme. Also provided herein are processes for preparing compounds described herein, inter- mediates used in their synthesis, pharmaceutical compositions thereof.

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

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IMPROVED AND SIMPLIFIED PROCESS FOR THE PREPARATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACID

A process for preparation of 1,2-benzisoxazole-3-acetic acid reacting 4-hydroxy coumarin and hydroxylamine in water according to the following scheme of reaction. Formula (I).

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Benzisoxazole – Wikipedia,
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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In a patent, 4865-84-3, molecular formula is C9H7NO3, introducing its new discovery. HPLC of Formula: C9H7NO3

1-PHENYL-SUBSTITUTED HETEROCYCLYL DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS

The present invention relates to 1-phenyl-substituted heterocyclyl derivatives of the formula (I), O Y R5 R6 N R2 R3 R4 X Z R1 R7 R7 R10 n (I) 5 wherein X, Y,Z,n,R1, R2, R3, R4, R5, R6, R7 and R10 are as described in the description and their use as prostaglandin receptor modulators, most particularly as prostaglandin D 2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.10

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

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Enantioselective nickel-catalyzed Michael additions of azaarylacetates and acetamides to nitroalkenes

Put a nickel in it: Azaarylacetates and acetamides, which have been neglected as substrates in catalytic asymmetric synthesis, undergo highly enantioselective Michael additions to nitroalkenes in the presence of a chiral nickel(II)-bis(diamine) complex (see scheme; Bn=benzyl, MS=molecular sieves). This process is tolerant of a wide variety of azaarenes in the pronucleophile. Copyright

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Benzisoxazole – Wikipedia,
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Process for the preparation of zonisamide

The present invention provides an improved process for the preparation of zonisamide or a derivative thereof comprising (a) reacting 1,2-benzisoxazole-3-methane-sulfonic acid with a halogenating agent in a first organic solvent to provide benzisoxazole methane sulfonyl halide; and, (b) reacting benzisoxazole methane sulfonyl halide with an amine in a second organic solvent to form zonisamide or a derivative thereof.

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Benzisoxazole – Wikipedia,
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METHODS FOR HAIR FOLLICLE STEM CELL PROLIFERATION

The present invention relates to compositions of Sonic Hedgehog (Shh) pathway activators and 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