50775-35-4

Upstream product

• 357-77-7 1,1-bis(4-fluorophenyl)prop-2-yn-1-ol 
• 1391868-38-4 C₁₈H₁₈F₂OSi 
• 118875-18-6 ethyl 2-cyano-3,3-bis(4-fluorophenyl)-2-propenoate 
• 50775-33-2 3,3-bis(4-fluorophenyl)-3-hydroxypropanenitrile 
• 2537-48-6 diethyl 1-cyanomethylphosphonate 
• 345-92-6 4,4'-Difluorobenzophenone 

Downstream Products

• 144477-59-8 3,3-bis(4-fluorophenyl)-2-propen-1-amine 
• 53017-84-8 2,2-bis(4-fluorophenyl)cyclopropanenitrile 
• 91472-94-5 3,3-bis(4-fluorophenyl)propan-1-amine 
• 50775-37-6 3,3-bis(4-fluorophenyl)propionitrile 

Relevant academic research and scientific papers

Cascade reaction of propargylic alcohols with hydroxylamine hydrochloride: facile synthesis of α,β-unsaturated oximes and nitriles

We have developed an easy and practical method for the synthesis of α,β-unsaturated oximes and nitriles from readily available propargylic alcohols with hydroxylamine hydrochloride (NH2OH·HCl) under metal-free conditions. By using or not using p-toluenesulfonyl chloride (p-TsCl) as the dehydrating promoter, the desired nitriles or oximes could be obtained, respectively via a three-step one-pot or two-step one-pot process in moderate to excellent yields with good functional group compatibility.

Silver-Catalyzed Long-Distance Aryl Migration from Carbon Center to Nitrogen Center

Selective cleavage of an inert C-C bond followed by C-O/N bond formation through a long-distance aryl migration from a carbon to a nitrogen center via Ag catalysis is reported. The migration products were easily converted into γ-hydroxy amines and tetrahy

Synthesis of acrylonitriles through an FeCl3-catalyzed domino propargylic substitution/aza-Meyer-Schuster rearrangement sequence

Nontoxic cyanide source: An unprecedented route to acrylonitriles by employing propargylic alcohols and para-tolylsulfonohydrazide as a combined cyano source has been developed (see scheme). This efficient and practical cyanation reaction proceeds through an FeCl3-catalyzed domino propargylic substitution/aza-Meyer-Schuster rearrangement sequence, the rearrangement process of which is reported for the first time. Copyright

Novel process for the synthesis of class I antiarrhythmic agent (±)-cibenzoline and its analogs

Synthesis of (±)-cibenzoline and its analogs has been achieved by a simple sequence of reactions. The diaryl cyanoolefin intermediate 3 could be prepared by Knoevenagel condensation of benzophenone with ethylcyanoacetate to form the tetra-substituted olefin intermediate 2 followed by Krapcho deethoxycarbonylation or from β-hydroxynitrile intermediate 2' followed by the elimination of hydroxyl group respectively. The 2,2- diphenylcyclopropanecarbonitrile 4 was synthesized from intermediate 3 by cyclopropanation, which was converted to (±)-2-(2,2-diphenylcyclopropyl)- 2-imidazoline 5 by reaction with ethylenediamine in the presence of a catalytic amount of sulfur. Moreover, the obtained 2-imidazolines were smoothly oxidized to the corresponding imidazoles 6 in good to moderate yields. Copyright Taylor & Francis Group, LLC.

N-SUBSTITUTED PYRIDINONE OR PYRIMIDINONE COMPOUNDS USEFUL AS SOLUBLE EPOXIDE HYDROLASE INHIBITORS

Disclosed are compounds of the formula (I) with the definitions of A1 D, Q, W, X, Y and Z as indicated in the description, which are active against soluble epoxide hydrolase (sEH), compositions thereof and methods of using and making same. (I)

Anticonvulsant and central nervous system-depressing bis(fluorophenyl)alkylamides and their uses

Bis(Fluorophenyl)alkylamides have been chemically synthesized which possess beneficial pharmacological properties (e.g., anticonvulsant activity) useful for the treatment of neurological diseases or disorders, such as, for example, epilepsy, convulsions, and seizure disorders. The preferred compounds of the invention also cause little sedation and have high therapeutic and protective indices in animal models of epilepsy. These compounds further possess long pharmacological half-lives, which, in practical clinical therapeutic application, should translate into once-a-day dosing, of great benefit to patients suffering from these diseases and/or disorders. These compounds may also be of further clinical utility in the treatment of other diseases and disorders of the central and peripheral nervous systems, or diseases or disorders affected by them, including, but not limited to, spasticity, skeletal muscle spasms and pain, restless leg syndrome, anxiety and stress, and bipolar disorder.

Agents for the treatment of overactive detrusor. IV. Synthesis and structure-activity relationships of cyclic analogues of terodiline

A series of pyrrolidine derivatives were synthesized and examined for inhibitory activity on detrusor contraction in vivo. Among those compounds, 5,5-dimethyl-2-(2,2-diphenylethyl)-3-isopropylidenepyrrolidine hydrochloride (41 · HCl), 2-(2,2-di(4-fluorophenyl)ethylene)-5,5-dimethyl-3-isopropylidenepyrrol idine hydrochloride (42 · HCl), (+)5,5-dimethyl-2-(N,N-diphenylaminomethyl)-3-isopropylidenepyrrolidin e hydrochloride (+)-(43a · HCl),(-)-5,5-dimethyl-2-(N,N-diphenylaminomethyl)-3-isopropylidenepyrr olidine hydrochloride (-)-(43a · HCl), and 2-(N,N-di(4-fluorophenyl)aminomethyl)-5,5-dimethyl-3-isopropylidenepyr rolidine methanesulfonate (43b · MsOH) showed stronger inhibitory activity on detrusor contraction than terodiline.

Synthesis and histamine H2 agonistic activity of arpromidine analogues: replacement of the pheniramine-like moiety by non-heterocyclic groups

Analogues of the potent histamine H2 agonist arpromidine, characterized by non-hetrocyclic groups (phenyl, cyclohexyl, alkyl) instead of the pheniramine-like portion, were prepared and tested for their H2 agonistic and H1 antagonistic activity in the isolated guiea pig right atrium and ileum, respectively.In the diphenylpropylguanidine series an increase in H2 agonistic potency resulted from mono- or difluorination at one or both phenyl rings in the meta and/or para position (pD2 7.75 vs pD2 = 7.15 for the unsubstituted parent compound).Compounds chlorinated atboth phenyl rings were considerably less potent.Highest combined H2 agonistic/H1 antagonistic potency was found in the 4-fluorophenyl series.The arpromidine analogue with cyclohexyl and methyl group instead of phenyl and pyridine ring proved to be 30 times more potent than histamine in the atrium.The H1 antagonistic potency in cyclohexyl compounds was lower than in the diaryl series.Thus, aromatic rings appear not to be required for high H2 agonistic potency but are useful for combined H2 agonistic/H1 antagonistic activity. histamine / H2 receptor / H2 agonist / arpromidine / impromidine / H1 antagonist / antihistamine