362-87-8

Upstream product

• 79-37-8 oxalyl dichloride 
• 6175-14-0 1,1-bis-(4-fluorophenyl)ethene 
• 390-61-4 ethyl 3,3-bis(4'-fluorophenyl)acrylate 
• 379-82-8 ethyl 3,3-bis(4-fluorophenyl)-3-hydroxypropanoate 
• 345-92-6 4,4'-Difluorobenzophenone 
• 337-70-2 3,3-bis-(4-fluoro-phenyl)-3-hydroxy-propionic acid 
• 120553-08-4 3,3-bis(4-fluorophenyl)acrylaldehyde 

Downstream Products

• 362-85-6 1,1-bis-(4-fluoro-phenyl)-2-(4-nitro-phenyl)-ethene 
• 342-75-6 3,3-bis(4-fluorophenyl)-propanoic acid 
• 23349-10-2 4,4'-(2-bromoethene-1,1-diyl)bis(fluorobenzene) 

Relevant academic research and scientific papers

A Weinreb Amide Based Building Block for Convenient Access to β,β-Diarylacroleins: Synthesis of 3-Arylindanones

Towards the synthesis of symmetrical and unsymmetrical β,β-diarylacroleins for assembling diarylmethine fragments present in biologically important molecules, we have developed a new Weinreb amide (WA) based building block, derived from propiolic acid. The WA functionality present in this compound allowed the sequential addition of various arylmagnesium bromide reagents in a controlled manner. The developed methodology for the access to β,β-diarylacroleins has been utilised for the synthesis of biologically important 3-arylindanone molecules. Synthesis of both symmetrical and unsymmetrical β,β-diarylacrolein and diarylmethine fragments, have been achieved via easily accessible and hitherto unknown Weinreb Amide (WA) based building block 11. The WA functionality allowed the sequential addition of nucleophiles such as arylmagnesium bromide in a controlled manner, which has enabled the synthesis of an important 3-arylindanone molecule.

Palladium-catalyzed intramolecular amidation of C(sp2)-H bonds: Synthesis of 4-aryl-2-quinolinones

Figure presented A catalytic synthetic approach for the synthesis of 2-quinolinone compounds through a Pd-catalyzed C(sp2)-H functionalization/intramolecular amidation sequence is described. The cyclization process efficiently proceeds in the p

Acylguanidines as bioisosteres of guanidines: NG-acylated imidazolylpropylguanidines, a new class of histamine h2 receptor agonists

N1-Aryl(heteroaryl)alkyl-N2-[3-(1H-imidazol-4-yl) propyl]guanidines are potent histamine H2-receptor (H2R) agonists, but their applicability is compromised by the lack of oral bioavailability and CNS penetration. To improve pharmacokinetics, we introduced carbonyl instead of methylene adjacent to the guanidine moiety, decreasing the basicity of the novel H2R agonists by 4-5 orders of magnitude. Some acylguanidines with one phenyl ring were even more potent than their diaryl analogues. As demonstrated by HPLC-MS, the acylguanidines (bioisosteres of the alkylguanidines) were absorbed from the gut of mice and detected in brain. In GTPase assays using recombinant receptors, acylguanidines were more potent at the guinea pig than at the human H2R. At the hH1R and hH3R, the compounds were weak to moderate antagonists or partial agonists. Moreover, potent partial hH4R agonists were identified. Receptor subtype selectivity depends on the imidazolylpropylguanidine moiety (privileged structure), opening an avenue to distinct pharmacological tools including potent H4R agonists.

(2S,4S)-4-FLUORO-1-[4-FLUORO-BETA-(4-FLUOROPHENYL)-L-PHENYLALANYL]-2-PYRROLIDINECARBONITRILE P-TOLUENESULFONIC ACID SALT AND ANHYDROUS CRYSTALLINE FORMS THEREOF

The present invention includes anhydrous crystalline forms of (2S,4S)-4-fluoro-1-[4-fluoro-β-(4-fluorophenyl)-L-phenylalanyl]-2-pyrrolidinecarbonitrile p-toluenesulfonic acid salt.