91566-20-0

Upstream product

• 123-54-6 acetylacetone 
• 6971-45-5 2-methoxyphenylhydrazine hydrochloride 
• 67-51-6 3,5-dimethyl-1H-pyrazole 
• 100-66-3 methoxybenzene 
• 10199-63-0 1-(3,5-dimethyl-1H-pyrazol-1-yl)ethanone 
• 5720-06-9 2-Methoxyphenylboronic acid 
• 57396-67-5 (2-methoxyphenyl)hydrazine hydrochloride 

Downstream Products

• 83430-99-3 2-(3,5-dimethyl-1H-pyrazol-1-yl)phenol 

Relevant academic research and scientific papers

Regioselective Ortho Amination of an Aromatic C-H Bond by Trifluoroacetic Acid via Electrochemistry

A trifluoroacetic acid-facilitated ortho amination of alkoxyl arene has been established via anodic oxidation in an undivided cell. In the absence of any additional metal or oxidant reagents, a series of aromatic and heteroaromatic amine derivatives have

Copper-catalyzed C–N cross-coupling of arylboronic acids with N-acylpyrazoles

A copper-catalyzed C–N bond forming reaction of arylboronic acids and N-acylpyrazoles was developed. This procedure used N-acetyl protected pyrazoles as starting material instead of free pyrazoles (NH). The reaction worked under neutral conditions and did not require any base or ligand. The reaction showed good functional group tolerance.

ANTITRICHOPHYTOSIS SOLUTION FOR EXTERNAL USE

According to the present invention, a topical liquid agent having antifungal activity against dermatophytes, and further high nail permeability can be provided. The topical liquid agent for nail and/or skin for prevention or treatment of dermatophytosis comprises a film-forming agent and a compound represented by the formula: wherein R1 represents a hydrogen atom, C1-6 alkyl, or trifluoromethyl, R2 represents a hydrogen atom, C1-6 alkyl, halogen, -COO(C1-6 alkyl), or (CH2)1-3COOR where R represents a hydrogen atom or C1-6 alkyl, R3 represents a hydrogen atom, C1-6 alkyl, amino, trifluoromethyl, or OR where R represents a hydrogen atom or C1-6 alkyl, R4 represents a hydroxyl group, R5 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, or halogen, R6 represents a hydrogen atom, C1-6 alkyl, trifluoromethyl, halogen, amino, -NRaRb, nitro, hydroxy-C1-6 alkyl, -CONRaRb, -COO(C1-6 alkyl), -COOH, -(CH2)1-3COOR, or ORa where R represents a hydrogen atom or C1-6 alkyl, Ra and Rb may be the same or different from each other, and each represent a hydrogen atom, C1-6 alkyl, or C1-6 acyl, R7 represents a hydrogen atom, C1-6 alkyl, -OR where R represents a hydrogen atom or C1-6 alkyl, or halogen, R8 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, amino, or nitro, or a salt thereof.

PATCH FOR ANTI-DERMATOPHYTOSIS

A patch for nails or skin for prevention or treatment of dermatophytosis, containing a layer including a pressure sensitive adhesive layer and a compound represented by the formula: wherein R1 represents hydrogen, C1-16 alkyl, or trifluoromethyl; R2 represents hydrogen, C1-6 alkyl, halogen, —COO(C1-6 alkyl), or (CH2)1-3COOR; R3 represents hydrogen, C1-6 alkyl, amino, trifluoromethyl, or OR; R4 represents hydroxyl; R5 represents hydrogen, C1-6 alkyl, hydroxyl, or halogen; R6 represents hydrogen, C1-6 alkyl, trifluoromethyl, halogen, amino, —NRaRb, nitro, hydroxy-C1-6 alkyl, —CONRaRb, —COO(C1-6 alkyl), —COOH, —(CH2)1-3COOR, or ORa (Ra and Rb each represents hydrogen, C1-6 alkyl, or C1-6 acyl); R7 represents hydrogen, C1-6 alkyl, —OR, or halogen; R8 represents hydrogen, C1-6 alkyl, hydroxyl, amino, or nitro; and R represents hydrogen or C1-6 alkyl; or a salt thereof.

ANTI-TRICHOPHYTIC ADHESIVE PATCH

According to the present invention, a patch for nail and/or skin having antifungal activity against dermatophytes, and having higher nail permeability can be provided. The patch for nail and/or skin for prevention or treatment of dermatophytosis comprises in a pressure sensitive adhesive layer a compound represented by the formula: wherein R1 represents a hydrogen atom, C1-6 alkyl, or trifluoromethyl; R2 represents a hydrogen atom, C1-6 alkyl, halogen, -COO(C1-6 alkyl), or (CH2)1-3COOR (R represents a hydrogen atom or C1-6 alkyl); R3 represents a hydrogen atom, C1-6 alkyl, amino, trifluoromethyl, or OR (R represents a hydrogen atom or C1-6 alkyl); R4 represents a hydroxyl group; R5 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, or halogen; R6 represents a hydrogen atom, C1-6 alkyl, trifluoromethyl, halogen, amino, -NRaRb, nitro, hydroxy-C1-6 alkyl, -CONRaRb, -COO(C1-6 alkyl), -COOH, -(CH2)1-3COOR, or ORa (R represents a hydrogen atom or C1-6 alkyl, Ra and Rb may be the same or different from each other, and each represent a hydrogen atom, C1-6 alkyl, or C1-6 acyl); R7 represents a hydrogen atom, C1-6 alkyl, -OR (R represents a hydrogen atom or C1-6 alkyl), or halogen; and R8 represents a hydrogen atom, C1-6 alkyl, a hydroxyl group, amino, or nitro, or a salt thereof.

Site-selective arene C-H amination via photoredox catalysis

Over the past several decades, organometallic cross-coupling chemistry has developed into one of the most reliable approaches to assemble complex aromatic compounds from preoxidized starting materials. More recently, transition metal-catalyzed carbon-hydrogen activation has circumvented the need for preoxidized starting materials, but this approach is limited by a lack of practical amination protocols. Here, we present a blueprint for aromatic carbon-hydrogen functionalization via photoredox catalysis and describe the utility of this strategy for arene amination. An organic photoredox-based catalyst system, consisting of an acridinium photooxidant and a nitroxyl radical, promotes site-selective amination of a variety of simple and complex aromatics with heteroaromatic azoles of interest in pharmaceutical research. We also describe the atom-economical use of ammonia to form anilines, without the need for prefunctionalization of the aromatic component.

Diazirines as potent electrophilic Nitrogen sources: Application to the synthesis of Pyrazoles

Even after more than 50 years since its discovery, the electrophilic potential of diazirines was never truly exploited. This longstanding limitation has been resolved. N-Monosubstituted diaziridines and hydrazones are obtained by nucleophilic additions. They release, under hydrolysis conditions, the corresponding monosubstituted hydrazines. The latter were converted to pyrazoles in high yields. The adamantanone can be recovered in 80-100% yields. This work demonstrates the potential of diazirines as electrophilic nitrogen sources with recoverable protecting groups.

TOPICAL LIQUID AGENT FOR THE TREATMENT OF DERMATOPHYTOSIS

A topical liquid agent for a nail and/or skin for prevention or treatment of dermatophytosis comprises a film-forming agent and a compound represented by the formula: wherein R1 represents hydrogen, C1-6 alkyl, or trifluoromethyl, R2 represents hydrogen, C1-6 alkyl, halogen, —COO(C1-6 alkyl), or (CH2)1-3COOR where R represents hydrogen or C1-6 alkyl, R3 represents hydrogen, C1-6 alkyl, amino, trifluoromethyl, or OR where R represents hydrogen or C1-6 alkyl, R4 represents hydroxyl, R5 represents hydrogen, C1-6 alkyl, hydroxyl, or halogen, R6 represents hydrogen, C1-6 alkyl, trifluoromethyl, halogen, amino, —NRaRb, nitro, hydroxy-C1-6 alkyl, —CONRaRb, —COO(C1-6 alkyl), —COOH, —(CH2)1-3COOR, or ORa where R represents hydrogen or C1-6 alkyl, Ra and Rb each represent hydrogen, C1-6 alkyl, or C1-6 acyl, R7 represents hydrogen, C1-6 alkyl, —OR where R represents hydrogen or C1-6 alkyl, or halogen, R8 represents hydrogen, C1-6 alkyl, hydroxyl, amino, or nitro, or a salt thereof.

TOPICAL ANTIFUNGAL AGENT

An anti-fungal agent for tinea comprising as active ingredient a compound having the skeleton of 2-(1H-pyrazol-1-yl)phenol represented by the following formula (I) or (II) or a salt thereof is provided