286441-91-6

Upstream product

• 2835-98-5 2-Hydroxy-4-methylanilin 
• 98-59-9 p-toluenesulfonyl chloride 
• 95-84-1 3-amino-4-hydroxytoluene 

Downstream Products

• 863301-17-1 4-toluenesulfonic acid 5-methyl-2-[(4-nitrophenyl)amino]phenyl ester 
• 286441-94-9 toluene-4-sulfonic acid 2-amino-2'-bromo-3',5'-dimethoxy-5-methyl-biphenyl-3-yl ester 
• 286441-95-0 toluene-4-sulfonic acid 6,8-dimethoxy-3-methyl-9H-carbazole-1-yl ester 
• 286441-93-8 toluene-4-sulfonic acid 2-amino-3',5'-dimethoxy-5-methyl-biphenyl-3-yl ester 
• 863301-19-3 N-[2-(trimethylsilyl)ethoxymethyl]-3-methyl-6-nitro-1-(4-toluenesulfonyloxy)carbazole 
• 863301-18-2 3-methyl-6-nitro-1-(4-toluenesulfonyloxy)carbazole 
• 863301-14-8 2-amino-2'-bromo-5-methyl-3-(4-toluenesulfonyloxy)-1,1'-biphenyl 
• 863301-15-9 2,2'-dibromo-5-methyl-3-(4-toluenesulfonyloxy)-1,1'-biphenyl 
• 286441-92-7 toluene-4-sulfonic acid 2-amino-3-bromo-5-methylphenyl ester 
• 863301-13-7 4-toluenesulfonic acid 2-amino-3-iodo-5-methylphenyl ester 

Relevant academic research and scientific papers

The first synthesis of clausenamine-A and cytotoxic activities of three biscarbazole analogues against cancer cells

Clausemine-A (3), isolated from the stem and root bark of Clausena excavata, was synthesized using Suzuki cross-coupling and Oxidative coupling as the key step. Compound 3, and the other two structurally related biscarbazoles 1 and 2, showed potent cytotoxic activities a variety of human cancer cell lines in vitro. (C) 2000 Elsevier Science Ltd. All rights reserved.

Phosphonic acid derivatives and application thereof

The invention belongs to the field of medical chemistry, relates to phosphonic acid derivatives for treating virus infectious diseases and an application thereof, and in particular, relates to the compounds represented by the formula (I) or isomers, pharmaceutically acceptable salts, solvates or prodrugs thereof, a preparation method thereof, pharmaceutical compositions containing the compounds and an application of the compounds or the compositions in preparation of drugs for treating the virus infection diseases.

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.

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.

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

One-step construction of carbazoles by way of the palladium-catalyzed double N-arylation reaction and its application to the total synthesis of murrastifoline-A

The one-step construction of N-substituted carbazoles by way of the Pd-catalyzed double N-arylation reaction of primary amines with 2,2′-dibromobiphenyl is described. Aryl and aliphatic amines including tert-butylamine and a protected glucopyranosylamine were effectively transformed into the corresponding N-substituted carbazoles. The first total synthesis of murrastifoline-A, a biscarbazole alkaloid, based on this methodology is also presented.

Total synthesis of murrastifoline-A by way of the Pd-catalyzed double N-arylation of a carbazolamine with a 2,2′-dibromobiphenyl derivative

The first total synthesis of murrastifoline-A (1), a biscarbazole alkaloid is described. The biscarbazole skeleton of 1 was effectively constructed by the Pd-catalyzed double N-arylation of carbazolamine (bottom-half segment, 3) with dibromobiphenyl deriv

Synthesis of optically pure Clausenamine-A and its demethoxylated analogs

The first total synthesis of Clausenamine-A (3) was developed involving the Suzuki cross-coupling and oxidative coupling reaction. The synthesis of its demethoxylated analogs 1 and 2 were also reported. Resolution of (+)-1, (+)-2, (+)-3 and (-)-1, (-)-2, (-)-3 were performed via their corresponding camphorsulfonates of the racemates. The absolute configurations of (+)-1, (+)-2, (+)-3 and (-)-1, (-)-2, (-)-3 were assigned as (aR) and (aS), respectively, by X-ray analysis and their CD spectrum. The primarily cytotoxic activities of these biscarbazoles against Plasmodium falciparum were briefly described. (C) 2000 Elsevier Science Ltd.