791-37-7

Upstream product

• 14746-54-4 4-dimethylamino-1,1-diphenyl-but-2-yn-1-ol 
• 7223-38-3 N,N-Dimethylpropargylamin 
• 119-61-9 benzophenone 
• 201230-82-2 carbon monoxide 
• 3923-51-1 1,1-diphenylprop-2-en-1-ol 
• 124-40-3 dimethyl amine 
• 109-54-6 3-(Dimethylamino)propyl chloride 

Downstream Products

• 4165-81-5 1,1-diphenyl-1,3-butadiene 
• 46970-87-0 DHP-362 

Relevant academic research and scientific papers

Tuning the reducing properties of 1,2-diaryl-1,2-disodiumethanes

(Chemical Equation Presented) We investigated the reducing properties of a series of 1,2-diaryl-1,2-disodiumethanes by means of equilibration reactions. The electron-donor power of these vic-diorganometals is strongly affected by the nature of substituents present either on the aromatic ring(s) or on the carbanionic centers, and it can be correlated with their ability to delocalize the arylmethyl carbanions. These findings are supported by electrochemical analysis of the reduction behavior of the parent 1,2-diarylalkene. Applications of these results to the reduction of selected substrates are described. 2009 American Chemical Society.

Discovery of diphenyl amine based sodium channel blockers, effective against hNav1.2

The development of new therapies for chronic pain is an area of unmet medical need. Central to pathways of chronic pain is the upregulation of voltage-gated sodium channels. The use of tricyclic antidepressants, which also have sodium channel activity, in chronic pain therapy prompted us to develop novel compounds from this scaffold. Herein, we show that the tricyclic moiety is not needed for effective inhibition of the [3H]-BTX binding site and sodium currents of hNav1.2. Our lead compound 6, containing a diphenyl amine motif, demonstrated a 53% inhibitory block of Nav1.2 currents at 10 μM, which is greater than 50% increase in current block in comparison to the amitriptyline standard. Altogether our study establishes that the tricyclic motif is unnecessary for hNav1.2 activity and modification of the amine portion is detrimental to sodium channel block.

NOVEL TRICYCLIC, BICYCLIC, MONOCYCLIC, AND ACYCLIC AMINES AS POTENT SODIUM CHANNEL BLOCKING AGENTS

The present invention provides acyclic, bicyclic, monocyclic, and tricyclic analogs and derivatives of tricyclic antidepressants which have sodium channel inhibiting activity. The compounds of the invention are useful as analgesics and anesthetics for diseases, conditions, and disorders where regulation of sodium channel activity can alleviate pain.

Regioselective hydroaminomethylation of 1,1-diaryl-allyl-alcohols: A new access to 4,4-diarylbutylamines

Pharmacologically active 4,4-diarylbutylamines like Fluspirilene and 4-amino-1,1-diarylbutan-1-ols like Difenidol were prepared in high yields via rhodium catalysed hydroaminomethylation of 1,1-diaryl-allylalcohols. Conversion of these olefins with carbon monoxide, hydrogen and secondary amines proceeds with complete regioselectivity. This group can easily be removed under acidic and hydrogenating conditions, enabling the transformation of 4-amino-1,1-diarylbutan-1-ols to 4,4-diarylbutylamines in high yields. Thus Fluspirilene was synthesised in 88% yield in four steps starting from commercially available materials. Graphical Abstract.