32686-54-7

Upstream product

• 67-66-3 chloroform 
• 108-42-9 3-chloro-aniline 
• 139-71-9 m-chloroformanilide 
• 4947-89-1 1-(3-chlorophenyl)-2-thiourea 
• 57668-47-0 (3-chlorophenyl)carbonimidic dichloride 

Downstream Products

• 74752-17-3 [1-Aziridin-1-yl-meth-(Z)-ylidene]-(3-chloro-phenyl)-amine 
• 74739-80-3 (3-Chloro-phenyl)-[1-pyrrolidin-1-yl-meth-(Z)-ylidene]-amine 
• 74755-76-3 (3-Chloro-phenyl)-[1-piperidin-1-yl-meth-(Z)-ylidene]-amine 
• 74739-42-7 (3-Chloro-phenyl)-[1-morpholin-4-yl-meth-(Z)-ylidene]-amine 
• 890966-18-4 C₁₅H₁₂Cl₃N₃O₂ 
• 1224234-84-7 6-chloro-2-(3-chlorophenyl)amino-3-phenylaminobenzofuran 
• 403813-69-4 1-(4-methoxybenzyl)-3-(3-chlorophenyl)thiourea 
• 405067-62-1 1-((benzo[d][1,3]dioxol-5-yl)methyl)-3-(3-chlorophenyl)thiourea 
• 109100-41-6 N-(3-chlorophenyl)piperidine-1-carbothioamide 
• 5330-63-2 t-butyl 3-chlorophenylcarbamate 

Relevant academic research and scientific papers

Design, synthesis and anticancer evaluation of 3-methyl-1H-indazole derivatives as novel selective bromodomain-containing protein 4 inhibitors

Bromodomain-containing Protein 4 (BRD4), an ‘epigenetic reader’, regulates chromatin structure and gene expression via recognizing and binding acetylated lysine in histones. BRD4 has become a therapeutic target for cancers because it promotes the expression of the tumor genes, such as c-Myc, NF-κB, and Bcl-2. In this study, a new series of 3-methyl-1H-indazole derivatives were designed via virtual screening and structure-based optimization. All compounds were synthesized and evaluated for their inhibitory activities to BRD4-BD1 and their antiproliferative effects in cancer cell lines. Among them, several compounds (such as 9d, 9u and 9w) exhibited strong BRD4-BD1 affinities and inhibition activities, and potently suppressed MV4;11 cancer cell line proliferation. Among them, compound 9d showed excellent selectivity for BRD4 and effectively suppressed c-Myc, the downstream protein of BRD4. This study provided new lead compounds for further biological evaluation on BRD4.

Visible-light-induced radical cascade cyclization of oxime esters and aryl isonitriles: Synthesis of cyclopenta[: B] quinoxalines

A visible-light-induced radical cascade cyclization of aryl isonitriles and cyclobutanone oxime esters for the synthesis of cyclopenta[b]quinoxalines has been accomplished for the first time. The key to the success of this process was the integration of the in situ-formed nitrile radical followed by the cascade radical isonitrile/nitrile insertion-cyclization. The easy introduction of substituents for both substrates and the high functional group tolerance of the reaction make it an efficient strategy to give various quinoxaline derivatives in moderate to good yields.

THERAPEUTIC COMPOUNDS AND USES THEREOF

The present invention relates to compounds useful in the modulation of ion channel activity in cells. The invention also relates to use of these compounds in the treatment of pain, and pharmaceutical compositions containing these compounds and methods for their preparation.

An isocyanide based multi-component reaction under catalyst- and solvent-free conditions for the synthesis of unsymmetrical thioureas

A new and efficient method for the synthesis of thiourea derivatives by a sequential one-pot, three-component reaction between aromatic isocyanides, amines, and 1,2-di-tert-butyldisulfane (DTBS) was developed and 27 different examples were synthesized in good to excellent yields. DTBS was identified as an effective sulfur surrogate without the use of both catalysts and solvents. This protocol does not employ any transition metal catalyst or special experimental setup.

Silver-Catalyzed Chemoselective [4+2] Annulation of Two Isocyanides: A General Route to Pyridone-Fused Carbo- and Heterocycles

A silver-catalyzed chemoselective [4+2] annulation of aryl and heteroaryl isocyanides with α-substituted isocyanoacetamides was developed for the facile and efficient synthesis of 2-aminoquinolones, naphthyridines, and phenanthrolines. A mechanism for this multistep domino reaction is proposed on the basis of a13C-labeling experiment, according to which an unprecedented chemoselective heterodimerization of two different isocyanides generates an α-amidoketenimine intermediate, which undergoes 1,3-amino migration to form an α-imidoylketene, followed by 6 π electrocyclization.

Novel ultrasound-promoted parallel synthesis of trifluoroatrolactamide library via a one-pot passerini/hydrolysis reaction sequence and their fungicidal activities

An ultrasound-promoted one-pot Passerini/hydrolysis reaction sequence has been developed for the synthesis of trifluoroatrolactamide derivatives using a diverse range of trifluoroacetophenones and isonitriles in acetic acid. Parallel synthesis in a centrifuge tube using a noncontact ultrasonic cell crusher was used in this study as an efficient method for the rapid generation of combinatorial trifluoroatrolactamide libraries, and subsequent biochemical evaluation of the resulting compounds indicated that they possessed excellent broad-spectrum fungicidal activities. N-(4-chlorophenyl)-2-(4-ethylphenyl)-3,3, 3-trifluoro-2-hydroxypropanamide and N-(4-chlorophenyl)-3,3,3-trifluoro-2- hydroxy-2-(4-methoxyphenyl)propanamide, in particular, showed significant fungicidal activities against all of the fungal species tested in the current study.

Oxidation of arylthiourea by cetyltrimethylammonium dichromate

With a view to investigate the oxidation behaviors of cetyltrimethylammonium dichromate on multifunctional groups, some arylthioureas were subjected to oxidation, both in neutral and in acidic conditions. In neutral conditions, the products were found to be a mixture of corresponding urea and isonitrile. In acidic conditions, the products were corresponding ureas only. A probable mechanism was proposed for the formation of the product, wherein the first step involves coupling of-NH2 and-SH of one molecule to the-NH2 and-SH of another molecule, respectively, which is followed by removal of nitrogen and sulfur. The microwave irradiation resulted in great yield of isonitrile than urea in neutral conditions. Supplemental materials are available for this article. Go to the publisher's online edition of Synthetic Communications to view the free supplemental file. Copyright Taylor & Francis Group, LLC.

Electrochemical generation of alkyl and aryl isocyanides

An efficient and widely applicable reagent-free method for the synthesis of alkyl and aryl isocyanides has been established. The electrochemical reduction of alkyl and aryl carbonimidoyl dichlorides under constant cathode potential leads to the corresponding isocyanides in almost quantitative yields. The availability of the starting materials, the mildness of the reaction conditions as well as the easy isolation of products are noteworthy, advantageous features of the procedure.