Brief introduction of 3-Chloro-1,2-benzisoxazole

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Benzisothiazole and benzisoxazole piperazine derivatives

Disubstituted N,N-piperazinyl derivatives are disclosed wherein one substituent is benzisothiazol-3-yl or benzisoxazol-3-yl and the other is alkylene attached to heterocycles such as azaspiro[4.5]decanedione, dialkylglutarimide, thiazolidinedione and spirocyclopentylthiazolidinedione or butyrophenone-like groups. The compounds have psychotropic properties and 8-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-8-azaspior[4.5]decane-7,9-dione is a typical embodiment having selective antipsychotic activity.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Synthesis of a bicyclic piperazine from l-aspartic acid and application of a fluoride-promoted SNAr coupling

The process development is reported of a pivotal C-N bond formation involving ((7R,9aS)-octahydro-1H-pyrido[1,2-a]pyrazin-7-yl)methanol (2) undergoing nucleophilic aromatic substitution with 3-chlorobenzo[d]isoxazole (3) to furnish ((7R,9aS)-2-(benzo[d]isoxazol-3-yl)octahydro-1H-pyrido[1,2-a] pyrazin-7-yl)methanol (4) as a key intermediate for a family of compounds (1). Essential to the success of the coupling is the use of fluoride in combination with a phase transfer catalyst. The development of an alternative route to bicyclic piperazine 2 that uses l-aspartic acid (20) as a starting material to avoid the need for a classical salt resolution is described.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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16263-52-8, 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, 16263-52-8, molecular formula is C7H4ClNO, introducing its new discovery.

3,8-DIAZA-BICYCLO[4.2.0]OCT-3-YL AMIDES

The present invention relates to 3,8-diaza-bicyclo[4.2.0]oct-3-yl amide derivatives of formula (I), wherein the relative configuration of the diazabicyclooctane moiety is cis; and wherein Ar1, and Ar2 are as described in the description, to their preparation, to pharmaceutically acceptable salts thereof, and to their use as pharmaceuticals, to pharmaceutical compositions containing one or more compounds of formula (I), and especially to their use as orexin receptor antagonists.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Method for treating allergies using substituted pyrazoles

A method for treating an allergic condition, including an atopic allergic condition, using substituted pyrazoles.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Properties and Exciting Facts About 3-Chloro-1,2-benzisoxazole

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Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase

This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Synthesis and inhibitory effects on platelet aggregation of 3-(2-thienyl)- and 3-(1-imidazolyl)-1,2-benzisoxazole derivatives

A series of 3-(2-thienyl)- and 3-(1-imidazolyl)-1,2-benzisoxazoles as well as some isomeric benzoxazoles were synthesized and tested in vitro for their inhibitory effect on arachidonic acid-induced human platelet aggregation.The most active compound (7-methoxy-3-(2-thienyl)-1,2-benzisoxazole 5c) was nearly 20-30-fold more potent than acetylsalicylic acid in inhibiting platelet aggregation.Structure-activity relationships within the series are briefly discussed. 1,2-benzisoxazole / platelet aggregation inhibitor

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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TRICYLIC DELTA 3-PIPERIDINES AS PHARMACEUTICALS

The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C 1-6alkanediyl; n is 1 or 2; X is–O–,–S–,–S(=O)–or–S(=O) 2–; each R 1is independently hydrogen, halogen, C 1-6alkyl, nitro, hydroxy or C 1-4alkyloxy; D is an indole, a benzisoxazole, a benzisothiazole, a 2H-benzopyranone, a phenoxyphenyl, a benzamide, a benzophenone or a benzopyrimidinone having central alpha 2-adrenoceptor antagonist activity. It further relates to their preparation, pharmaceutical use and compositions.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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OXINDOLE SUBSTITUTED PIPERAZINE DERIVATIVES

The invention relates to compounds of the formula (I), wherein Ar, A, R, R1, R2, R3, R4 and R5 are defined as in the specification, pharmaceutical compositions containing them and their use in the treatment of central nervous system disorders.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Photochemistry of matrix-isolated 3-chloro-1,2-benzisoxazole: Generation and characterization of 2-cyanophenoxyl radical and other reactive intermediates

Photochemistry of 3-chloro-1,2-benzisoxazole 1 in N2 and Ar matrices at 10 K leads to N-chloro-ketenimine 3 and 2-cyanophenyl-hypochlorite 4. The reaction kinetics and the observed photoisomerization of 3 to 4 indicate that ketenimine 3, possibly formed via an elusive vinylnitrene VN, is an intermediate in the formation of hypochlorite 4. A new pathway involving the formation of 2-cyanophenoxyl radical 5, which was captured only in Ar matrix, was also observed. Radical 5 is possibly formed via photodetachment of Cl atom from 1 (or VN) and might explain the formation of 3-chloro-6-oxocyclohexa-1,4-dienecarbonitrile 2 in N2 and Ar matrices. All the species were characterized by IR spectroscopy and theoretical calculations. The computed geometric and electronic structure of radical 5 is discussed. Overall, the results provided further insight into the mechanism of the photochemistry of 1,2-benzisoxazoles and allowed characterization of new interesting reactive intermediates.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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3-O-HETEROARYL-INGENOL

The present invention relates to a compound according to formula (I) wherein R1 represents optionally substituted heteroaryl, and pharmaceutically acceptable salts, hydrates, solvates or pharmaceutically acceptable and physiologically cleavable esters thereof. The invention relates further to intermediates for the preparation of said compounds, to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. diseases associated with hyperplasia, neoplasia or dysplasia, with said compounds, to methods of treatment of cosmetic indications with said compounds, and to the use of said compounds in the manufacture of medicaments.

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