247091-95-8

Upstream product

• 247092-11-1 2,4-difluoro-benzaldehyde oxime 
• 1550-35-2 2,4-difluorobenzaldehyde 

Downstream Products

• 159693-18-2 methyl 5-(chlorodifluoromethyl)-3-(2,4-difluorophenyl)-4-isoxazolecarboxylate 
• 159693-94-4 5-(chlorodifluoromethyl)-3-(2-fluoro-4-hydroxy-5-nitrophenyl)-4-isoxazolecarboxamide 
• 159693-93-3 5-(chlorodifluoromethyl)-3-(2-fluoro-4-methoxy-5-nitrophenyl)-4-isoxazolecarboxamide 
• 159693-92-2 5-(chlorodifluoromethyl)-3-(2-fluoro-4-methoxy-5-nitrophenyl)-4-isoxazolecarboxylic acid 
• 159693-89-7 methyl 5-(chlorodifluoromethyl)-3-(2,4-difluoro-5-nitrophenyl)-4-isoxazolecarboxylate 
• 159693-91-1 5-(chlorodifluoromethyl)-3-(2-fluoro-4-methoxy-5-nitrophenyl)-4-isoxazolecarboxylic acid methyl ester 
• 159693-95-5 4-<4-(aminocarbonyl)-5-(chlorodifluoromethyl)-3-isoxazolyl>-5-fluoro-2-nitrophenoxyacetic acid ethyl ester 
• 334971-41-4 3-(2,4-difluoro-phenyl)-5-methyl-isoxazole-4-carboxylic acid ethyl ester 
• 1309794-05-5 (R)-2-(3-(2,4-difluorophenyl)-4,5-dihydroisoxazol-5-yl)acetic acid 
• 1309794-06-6 (R)-2-(3-(2,4-difluorophenyl)-4,5-dihydroisoxazol-5-yl)-1-morpholinoethanone 
• 1309794-04-4 (1R,2S)-2-phenylcyclohexyl 2-((R)-3-(2,4-difluorophenyl)-4,5-dihydroisoxazol-5-yl)acetate 
• 897645-82-8 5-amino-3-(2,4-difluorophenyl)-4-(4-pyrimidinyl)isoxazole 

Relevant academic research and scientific papers

Palladium-Catalyzed Cyclization Reaction of Oxime Acetates and Aryl Iodides: Syntheses of 2-Imidazolines

A novel and versatile method for the synthesis of 2-imidazolines has been developed via the Pd-catalyzed cyclization reaction of readily available homoallenyl oxime acetates with aryl iodides. This protocol is performed under mild reaction conditions and needs no additives or ligands.

Triazole alcohol derivative as well as preparation method and application thereof

The invention relates to a triazole alcohol derivative as well as a preparation method and application thereof. The chemical structure of the triazole alcohol derivative is shown as a formula I, R1 represents a benzene ring or a substituted benzene ring, and substituent groups of the substituted benzene ring can be located at all positions of the benzene ring, can be mono-substituted or multi-substituted, and can be selected from a) halogen which is F and Cl; b) an electron withdrawing group which is cyano or trifluoromethyl; c ) a lower alkyl of 1-4 carbon atoms or a halogen substituted loweralkyl; and d) lower alkoxy of 1-4 carbon atoms or halogen substituted lower alkoxy. The compound of the invention has strong antifungal activity, has the advantages of low toxicity, wide antibacterial spectrum and the like, and can be used for preparing antifungal drugs.

Design, synthesis, and in vitro evaluation of novel triazole analogues featuring isoxazole moieties as antifungal agents

In order to develop novel antifungal agents, based on our previous work, a series of (2R,3R)-3-((3-substitutied-isoxazol-5-yl)methoxy)-2-(2,4-difluorophenyl)-1-(1H-1,2,4-triazol-1-yl) butan-2-ol (a1-a26) were designed and synthesized. All of the compounds exhibited good in vitro antifungal activities against eight human pathogenic fungi. Among them, compound a6 showed excellent inhibitory activity against Candida albicans and Candida parasilosis with MIC80 values of 0.0313 μg/mL. In addition, compounds a6, a9, a12, a13 and a14 exhibited moderate inhibitory activities against fluconazole-resistant isolates with MIC80 values ranging from 8 μg/mL to 16 μg/mL. Furthermore, compounds a6, a12 and a23 exhibited low inhibition profiles for CYP3A4. Clear SARs were analyzed, and the molecular docking experiment was carried out to further investigate the relationship between a6 and the target enzyme CYP51.

Design, synthesis, and in vitro evaluation of novel antifungal triazoles

Twenty-nine novel triazole analogues of ravuconazole and isavuconazole were designed and synthesized. Most of the compounds exhibited potent in vitro antifungal activities against 8 fungal isolates. Especially, compounds a10, a13, and a14 exhibited superior or comparable antifungal activity to ravuconazole against all the tested fungi. Structure-activity relationship study indicated that replacing 4-cyanophenylthioazole moiety of ravuconazole with fluorophenylisoxazole resulted in novel antifungal triazoles with more effectiveness and a broader-spectrum.

Triazole alcohol derivative and preparation method and application thereof

The invention relates to a triazole alcohol derivative and a preparation method and application thereof. The chemical structure of the triazole alcohol derivative is as shown in the formula I. The invention also provides salt of the compound, a pharmaceutical composition, a preparation method and application. The compound of the invention has strong antifungal activity, has advantages of low toxicity and wide antimicrobial spectrum, and can be used for preparation of antifungal drugs.

AMINOBENZISOXAZOLE COMPOUNDS AS AGONISTS OF A7-NICOTINIC ACETYLCHOLINE RECEPTORS

The present invention relates to novel aminobenzisoxazole compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ot7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.

CHIRAL SYNTHESIS OF ISOXAZOLINES, ISOXAZOLINE COMPOUNDS, AND USES THEREOF

Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.

ISOXAZOLE-PYRIDINE DERIVATIVES

The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A α5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.

Compounds and method for inhibiting MRP1

The present invention relates to a compound of formula (I), which is useful for inhibiting resistant neoplasms where the resistance is conferred in part or in total by MRP1.

Synthesis and Herbicidal Activity of 3-Aryl-5-(haloalkyl)-4-isoxazolecarboxamides and Their Derivatives

A series of unique 3-aryl-5-(haloalkyl)-4-isoxazolecarboxamides have been prepared which exhibit, in both greenhouse and field studies, significant preemergent and postemergent herbicidal activity in the grams per hectare range against broadleaf and narro