98586-21-1

Upstream product

• 1073-06-9 3-fluorobromobenzene 
• 109-94-4 formic acid ethyl ester 
• 345-70-0 3,3'-difluorobenzophenone 
• 456-48-4 3-Fluorobenzaldehyde 
• 1224964-62-8 3,3'-difluorobenzhydryl tosylate 
• 107337-71-3 3-fluorophenyllithium 

Downstream Products

• 98586-06-2 bis(3-fluorophenyl)methane 
• 345-70-0 3,3'-difluorobenzophenone 
• 508211-20-9 methyl 2-[bis(3-fluorophenyl)methoxy]-5-nitrobenzoate 
• 1207274-75-6 carbonic acid (R)-1-aza-bicyclo[2.2.2]oct-3-yl ester bis-(3-fluoro-phenyl)-methyl ester 
• 1404054-70-1 (3R)-1-benzyl-3-((bis(3-fluorophenyl)methoxy)-carbonylamino)-1-methylpyrrolidinium iodide 
• 1404055-13-5 bis(3-fluorophenyl)methyl 1-methylpiperidine-4-carboxylate 
• 1404054-23-4 bis(3-fluorophenyl)methyl quinuclidine-3-carboxylate 
• 10605-49-9 1,1-bis(3-fluorophenyl)ethylene 
• 117082-80-1 C₁₅H₁₂F₂O₂S 
• 117082-83-4 2-((bis(3-fluorophenyl)methyl)thio)acetamide 
• 117082-77-6 2-((bis(3-fluorophenyl)methyl)sulfinyl)acetamide 
• 1404054-68-7 (R)-3-((bis(3-fluorophenyl)methoxy)carbonothioylamino)-1-(2-oxo-2-(thiophen-2-yl)ethyl)-1-azoniabicyclo[2.2.2]octane chloride 
• 1404054-53-0 (R)-3-((bis(3-fluorophenyl)methoxy)carbonyl amino)-1-(2-(2,3-dihydrobenzofuran-5-yl)ethyl)-1-azoniabicyclo[2.2.2]octane bromide 
• 1404054-16-5 (R)-bis(3-fluorophenyl)methyl quinuclidin-3-ylcarbamate 

Relevant academic research and scientific papers

Temperature-controlled divergent synthesis of 4-alkoxy- or 4-alkenyl-chromanes via inverse electron-demand cycloaddition with in situ generated ortho-quinone methides

The temperature-controlled divergent synthesis of 4-alkoxy- or 4-alkenyl-chromanes via inverse electron-demand cycloaddition with in situ generated ortho-quinone methides under identical reaction conditions except for thermal condition has been developed. At room temperature, the reaction generated 4-methoxychromanes, whereas the reaction performed at room temperature to 100 °C gave 4-alkenylchromanes. Trifluoromethanesulfonic acid was efficiently suitable in the reaction to give the 4-substituted chromanes. This divergent synthetic strategy exhibits a new method giving carbon–carbon or carbon–oxygen bond by controlling the reaction temperature.

Direct allylation of benzyl alcohols, diarylmethanols, and triarylmethanols mediated by XtalFluor-E

We report the direct allylation of benzyl alcohols, diarylmethanols and triarylmethanols mediated by XtalFluor-E using allyltrimethylsilane. The resulting allylated products are obtained in moderate to high yield.

Kinetics of the solvolyses of fluoro-substituted benzhydryl derivatives: Reference electrofuges for the development of a comprehensive nucleofugality scale

A series of m-fluoro-substituted benzhydryl chloridcjs, bromides, mesylates and Losylates 1-X to 5-X were prepared and subjected to solvolysis reactions in various solvents. The observed first-order rate constants ks(25 °C) were found to follow the correlation equation log ks(25 °C) = Sf(Nf + Ef), which allowed us to determine the electrofugalily parameters Ef for these destabilized benzhydrylium cations and the nucleofugality parameters Nf, S f for a series of leaving group/ solvent combinations.

MODULATORS OF C3A RECEPTOR AND METHODS OF USE THEREOF

Provided are compounds that are modulators of C3a receptor activity, compositions containing the compounds and methods of use of the compounds and compositions. In certain embodiments, the compounds are pyridones. In certain embodiments, provided are methods for treatment or amelioration of diseases associated with modulation of C3a receptor activity.

Novel inhibitors of the gardos channel for the treatment of sickle cell disease

Sickle cell disease (SCD) is a hereditary condition characterized by deformation of red blood cells (RBCs). This phenomenon is due to the presence of abnormal hemoglobin that polymerizes upon deoxygenation. This effect is exacerbated when dehydrated RBCs experience a loss of both water and potassium salts. One critical pathway for the regulation of potassium efflux from RBCs is the Gardos channel, a calcium-activated potassium channel. This paper describes the synthesis and biological evaluation of a series of potent inhibitors of the Gardos channel. The goal was to identify compounds that were potent and selective inhibitors of the channel but had improved pharmacokinetic properties compared to 1, Clotrimazole. Several triarylamides such as 10 and 21 were potent inhibitors of the Gardos channel (IC50 of 10 nM) and active in a mouse model of SCD. Compound 21 (ICA-17043) was advanced into phase 3 clinical trials for SCD.

Dications of fluorenylidenes. The relationship between redox potentials and antiaromaticity for meta- and para-substituted diphenylmethylidenefluorenes

Electrochemical oxidation of meta-substituted diphenylmethylidenefluorenes (3a-g) results in the formation of fluorenylidene dications that are shown to be antiaromatic through calculation of the nucleus independent chemical shift (NICS) for the 5- and 6-

BENZENE DERIVATIVES,PROCESS FOR PREPARING THE SAME AND USE THEREOF

Novel benzene derivatives represented by the formula (I) : wherein R1, R4 and R6 each independently represents a hydrogen atom, a halogen atom or a hydrocarbon group, R2 represents a hydrocarbon group or a heterocyclic group, R3 represents a hydrocarbon group, NR7'R7 or OR8 (wherein R7' represents a hydrogen atom or a hydrocarbon group, R7 represents a non-aromatic group, or R7' and R7 may form a ring with the adjacent nitrogen atom, and R8 represents a hydrocarbon group or a heterocyclic group), R5 represents a hydrocarbon group or a heterocyclic group (except for a quinolyl group), R5' represents a hydrogen atom, or a hydrocarbon group, or R5 and R5' may form a ring with the adjacent nitrogen atom, and R5" represents a hydrogen atom or a hydrocarbon group, which have vanilloid receptor agonist activity and are useful as a drug such as an analgesic and an agent for preventing and/or treating urinary frequency and/or urinary incontinence.

Fused-ring compounds and use thereof as drugs

The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. Th

Tricyclic compounds, their production and use

A compound of the formula: wherein R1 is H or a substituent; m is 1-3; Ar is an aromatic group which may be substituted; X is a bond or a divalent straight-chain group having 1-6 atoms which may be substituted; Y is —S—, —O—, or —N(R2— (R2 is H or a substituent group), Z is —N= or —C(R3)= (R3 is H or a hydrocarbon group), ring A is a benzene ring; ring B is a 5- to 7-membered ring which may be substituted, or a salt thereof is useful for eliciting a prostaglandin I2 receptor agonistic effect.

3'-Chloro-3α-(diphenylmethoxy)tropane but not 4'-chloro-3α- (diphenylmethoxy)tropane produces a cocaine-like behavioral profile

A series of 2'- and 3'-substituted and 3',3''-disubstituted 3α- (diphenylmethoxy)tropane analogs were designed and synthesized as novel probes for the dopamine transporter. All the analogs were evaluated for displacement of [3H]WIN 35,428 binding at the dopamine transporter and for inhibition of [3H]dopamine uptake in rat caudate putamen. Compounds were observed to monophasically displace [3H]WIN 35,428 binding to the dopamine transporter with affinities of 21.6-1836 nM (K(i)). Generally, meta- substituted compounds were more potent than benztropine and equipotent to or slightly less potent than their previously reported parasubstituted homologs in inhibiting [3H]WIN 35,428 binding. However, these same metasubstituted analogs were typically less potent than the 4'-substituted analogs in inhibiting [3H]dopamine uptake. Ortho-substituted analogs were generally less potent in both binding and inhibition of uptake at the dopamine transporter than either benztropine or other aryl-substituted homologs. The analogs were also tested for binding at norepinephrine and serotonin transporters as well as muscarinic m1 receptors. None of the compounds in the present study bound with high affinity to either the norepinephrine or serotonin transporters, but all bound to muscarinic m1 receptors with high affinity (K(i) = 0.41-2.52 nM). Interestingly, 3'-chloro-3α- (diphenylmethoxy)tropane (5c) produced effects like cocaine in animals trained to discriminate 10 mg/kg cocaine from saline, unlike its 4'-Cl homolog and all of the previously evaluated benztropine analogs. Further evaluation of compound 5c and the other benztropine analogs will undoubtedly prove useful in the elucidation of the role of the dopamine transporter in the reinforcing effects of cocaine and the ultimate identification of a cocaine-abuse treatment.