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Condensation reactions of various nucleophiles with 3-formylchromone

3-Formylchromones 1 are condensed with 1-(2,4-difluorophenyl-2-[1,2,4] tnazol-4-yl)ethanone in acetic anhydride to afford 3-[3-(2,4-difluoro-phenyl)-3- oxo-2-[1,2,4]triazol-4-yl)propenyl]chromon-4-ones 2. 3-Formylchromone 1 when heated with benzo[d]isoxazol-3-yl-acetic acid in dry pyridine yield 3-(2-benzo[d]isoxazol-3-yl-vinyl)chromon-4-ones 3. Further, 3-formylchromone 1 on heating with N-methylpiperizine in ethanol give 1-(2-hydroxyphenyl)-3-(4- methyl-piperazin-1-yl)propenones 4.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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METHOD FOR SULFONATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACID

An efficient method for the preparation of 1,2-benzisoxazole-3-methanesulfonic acid involves a reaction of 1,2-benzisoxazole-3-acetic acid in toluene with chlorosulfonic acid optionally mixed with an inert solvent in the presence of a particular Lewis base (ester or a nitrile).

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Synthesis, anti-bacterial, anti-asthmatic and anti-diabetic activities of novel N-substituted-2-(benzo[d]isoxazol-3-ylmethyl)-1H-benzimidazoles

(Chemical Equation Presented) Synthesis of a series of novel class of N-substituted-2-(benzo[d]isoxazol-3-ylmethyl)-1H-benzimidazoles (4) by the condensation of o-phenylenediamine (1) with benzo[d]isoxazol-3-yl-acetic acid (2) and subsequent reactions with different types of electrophiles have been reported. Some compounds exhibited promising anti-bacterial activity against Salmonella typhimurium, however poor activity against Staphylococcus aureus. The compound 4t was found to have high activity even at 1 mug/ml compared to Cephalexin against S. aureus. The biological activity against PDE-IV for potential anti-asthmatic effect and against DP-IV and PTP-1B for potential anti-diabetic effects was disappointing.

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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

Brief introduction of 1,2-Benzisoxazole-3-acetic Acid

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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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Benzisoxazole – Wikipedia,
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Process for the preparation of 1,2-benzisoxazole-3-acetic acid

The present invention provides a process for preparing 1,2-benzisoxazole-3-acetic acid, comprising the step of reacting 4-hydroxy-coumarin with hydroxyl-amine in the presence of a base. The present invention further provides a process for preparing a salt of benzisoxazole methane sulfonic acid, comprising the steps of 1) sulfonating 1,2-benzisoxazole-3-acetic acid using chlorosulfonic acid in a solvent mixture comprising methylene chloride and sodium hydroxide; and 2) isolating the salt of benzisoxazole methane sulfonic acid.

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Benzisoxazole – Wikipedia,
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NOVEL OXABISPIDINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CARDIAC ARRHYTHMIAS

There is provided compounds of formula (I), wherein R1, R2, R3, R4, R 41 to R46, A, B and G 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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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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Process for the preparation of zonisamide and the intermediates thereof

The present invention provides a novel and improved process for the preparation of Zonisamide and the intermediates thereof. In one aspect of the present invention, the process provides for: the preparation and isolation of a novel crystalline form of anhydrous 1,2-benzisoxazole-3-methanesulfonic acid of formula 1; the direct chlorination of the acid of formula 1 into its acid chloride of formula 2; and the in situ conversion of the intermediate acid chloride of formula 2 into Zonisamide.

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Benzisoxazole – Wikipedia,
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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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Benzisoxazole – Wikipedia,
Benzisoxazole – an overview | ScienceDirect Topics

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SYNTHESIS OF 4-OXO-4H-BENZISOXAZOLO<2,3-a>PYRIDINES VIA DIMERIZATION OF 1,2-BENZISOXAZOLE-3-ACETIC ACIDS

Reactions of 1,2-benzisoxazole-3-acetic acid (1) with tosyl chloride and acyl chlorides in pyridine afforded the corresponding 4-oxo-4H-benzisoxazolo<2,3-a>pyridines (2).KEYWORDS – 1,2-benzisoxazole-3-acetic acids; dimerization; mixed anhydrides; tosyl chloride; N-C bond formation; 4-oxo-4H-benzisoxazolo<2,3-a>pyridines

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