26946-70-3

Upstream product

• 100-01-6 4-nitro-aniline 
• 571178-48-8 N¹-(2-aminophenyl)-N²-(4-nitrophenyl)thiourea 
• 95-54-5 1,2-diamino-benzene 
• 2131-61-5 p-nitrophenyl isothiocyanate 
• 1056477-06-5 2-bromocyclohexanone 
• 5901-56-4 N-4-nitrophenylguanidine 
• 4857-06-1 2-chloro-1H-benzoimidazole 

Downstream Products

• 1353676-90-0 1-(4-nitrophenyl)-2,3-dihydro-1H-imidazo[1,2-a]benzimidazole 
• 133929-18-7 2-(4-aminophenylamino)benzimidazole 
• 133929-20-1 2-(4-isothiocyanatophenylamino)benzimidazole 

Relevant academic research and scientific papers

Structure-Guided Development of Small-Molecule PRC2 Inhibitors Targeting EZH2-EED Interaction

Disruption of EZH2-embryonic ectoderm development (EED) protein-protein interaction (PPI) is a new promising cancer therapeutic strategy. We have previously reported the discovery of astemizole, a small-molecule inhibitor targeting the EZH2-EED PPI. Herein, we report the cocrystal structure of EED in complex with astemizole at 2.15 ?. The structure elucidates the detailed binding mode of astemizole to EED and provides a structure-guided design for the discovery of a novel EZH2-EED interaction inhibitor, DC-PRC2in-01, with an affinityKdof 4.56 μM. DC-PRC2in-01 destabilizes the PRC2 complex, thereby leading to the degradation of PRC2 core proteins and the decrease of global H3K27me3 levels in cancer cells. The proliferation of PRC2-driven lymphomas cells is effectively inhibited, and the cell cycle is arrested in the G0/G1 phase. Together, these data demonstrate that DC-PRC2in-01 could be an effective chemical probe for investigating the PRC2-related physiology and pathology and providing a promising chemical scaffold for further development.

Potassium Periodate Mediated Oxidative Cyclodesulfurization toward Benzofused Nitrogen Heterocycles

A convenient oxidative cyclodesulfurization method toward the synthesis of benzofused nitrogen heterocycles using inexpensive and readily available potassium periodate as an oxidant was developed. Upon treating isothiocyanates with ortho -substituted anilines bearing N, N -, N, O -, and N, S -bis-nucleophiles, followed by an intramolecular cyclization of the in situ generated monothioureas, substituted 2-aminobenzazole series were rapidly accessible in good to excellent yields. The protocol can accommodate various substituents on both substrates while allowing more efficient, greener, and operational simpler process relative to other oxidative coupling reactions. Tetracyclic quinazolinone derivatives were also afforded in high yields in a single preparative step and chromatography-free.

Ultrasound-assisted synthesis of substituted 2-aminobenzimidazoles, 2-aminobenzoxazoles, and related heterocycles

A sonochemical method for the synthesis of 2-aminobenzimidazoles and 2-aminobenzoxazoles, as well as chiral aminooxazolines and a chiral substituted quinazolin-5-one is reported. Using the Ph3P–I2system in the presence of triethylami

A new NBS/oxone promoted one pot cascade synthesis of 2-aminobenzimidazoles/2-aminobenzoxazoles: A facile approach

A new strategy for the synthesis of 2-aminobenzimidazoles via a reaction of α-halogenated cyclohexanone with guanidine is reported. It provides a facile N-bromosuccinimide (NBS) mediated transition metal free, sustainable path for the synthesis of 2-substituted azoles. NBS along with the oxone promotes in situ halogenation of cyclohexanone, which in turn, when allowed to react with guanidine, afforded 2-aminobenzimidazoles (2-ABI). This eco-friendly protocol provides a competent laboratory synthesis method associated with significant advantages such as greater selectivity, cost-efficiency, mild reaction conditions, absence of chromatographic purification, clean reaction profile, and a simple work-up procedure to furnish high yields. The structures of all the synthesized compounds were confirmed on the basis of IR, 1H and 13C NMR, mass spectrometry, and elemental analyses data. In addition, we have also extended the scope of this strategy for obtaining 2-amino substituted benzoxazoles.

FUSED HETEROCYCLIC COMPOUNDS

The present invention provides a compound which has the effect of PDE inhibition, and which is useful as an agent for preventing or treating schizophrenia. The compound is represented by the formula (I): wherein the symbols are defined in the specification.

A one-pot method for the synthesis of 2-aminobenzimidazoles and related heterocycles

A rapid and efficient one-pot method for the synthesis of 2-aminobenzimidazoles and related heterocycles is described. The reaction is mediated by a polymer-supported carbodiimide, which simplifies product isolation. The scope and limitations of this method are described.

Synthesis of Unsymmetrical Diheteroarylbenzenes: Benzoazole and Quinazoline Derivatives

Four different types of structures, namely 8, 14, 17 and 18 have been prepared for the first time.No more than five steps are needed to synthesize them using 4-nitroaniline as starting material.In order to confirm the proposed structures, some independent