216368-49-9

Upstream product

• 2417-73-4 methyl 2-bromomethylbenzoate 
• 122-52-1 triethyl phosphite 
• 1137728-03-0 C₅H₁₂IO₃PZn 
• 610-97-9 o-iodo-methyl-benzoic acid 
• 89-71-4 2-Methyl-benzoic acid methyl ester 

Downstream Products

• 1966-89-8 2-[2-(thienyl)vinyl] benzoic acid 
• 137349-02-1 diethyl 2-carboxybenzylphosphonate 
• 622393-88-8 2-(diethoxy-phosphorylmethyl)-benzoic acid 2-trimethylsilanyl-ethyl ester 
• 1622-55-5 9,10-dihydro-4H-benzo<4,5>cyclohepta<1,2-b>thiophen-4-one 
• 1622-54-4 2-[2-(thienyl)ethyl] benzoic acid 
• 1259374-15-6 ethyl 2-[(E)-2-(5-bromo-3-tert-butyl-2-methoxy-phenyl)-vinyl]-benzoate 
• 1313547-38-4 methyl 2-[(E)-non-1-enyl]benzoate 
• 1313547-40-8 2-[(E)-1-(diethylphosphono)non-1-enyl]benzoic acid 
• 13893-39-5 2-hexyldec-2-enal 
• 1313547-42-0 2-[(E)-1-diethylphosphono-2-phenylethen-1-yl]benzoic acid 
• 38453-72-4 (E)-methyl 2-styrylbenzoate 
• 1313547-39-5 methyl 2-[(E)-3,3-dimethylbut-1-enyl]benzoate 
• 1313547-41-9 2-[(E)-1-(diethylphosphono)pent-1-enyl]benzoic acid 
• 95330-34-0 methyl (E)-2-(pent-1-en-1-yl)benzoate 

Relevant academic research and scientific papers

Target hopping as a useful tool for the identification of novel EphA2 protein-protein antagonists

Lithocholic acid (LCA), a physiological ligand for the nuclear receptor FXR and the G-protein-coupled receptor TGR5, has been recently described as an antagonist of the EphA2 receptor, a key member of the ephrin signalling system involved in tumour growth. Given the ability of LCA to recognize FXR, TGR5, and EphA2 receptors, we hypothesized that the structural requirements for a small molecule to bind each of these receptors might be similar. We therefore selected a set of commercially available FXR or TGR5 ligands and tested them for their ability to inhibit EphA2 by targeting the EphA2-ephrin-A1 interface. Among the selected compounds, the stilbene carboxylic acid GW4064 was identified as an effective antagonist of EphA2, being able to block EphA2 activation in prostate carcinoma cells, in the micromolar range. This finding proposes the "target hopping" approach as a new effective strategy to discover new protein-protein interaction inhibitors. Target hopping: Given the ability of lithocholic acid to recognize FXR, TGR5 and EphA2 receptors, we hypothesized the structural requirements to bind each of these receptors might be similar. We selected a set of commercially available FXR or TGR5 ligands and tested them for their ability to inhibit EphA2 by targeting the EphA2-ephrin-A1 interface. Moreover, a small panel of GW4064 derivatives was synthesized. Copyright

TETRAAZA-CYCLOPENTA[A]INDENYL AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS

The present invention provides compounds of Formula (I) as M1 receptor positive allosteric modulators for the treatment of diseases mediated by the muscarinic M1 mediator.

Alkenylphosphonates: Unexpected products from reactions of methyl 2-[(diethoxyphosphoryl)methyl]benzoate under Horner-Wadsworth-Emmons conditions

Methyl 2-[(diethoxyphosphoryl)methyl]benzoate reacts with several aldehydes to produce an alkenylphosphonate as the major product, together with varying amounts of the expected Horner-Wadsworth-Emmons product, a 1,2-disubstituted E-alkene. Use of a bulky aldehyde or the tert-butyl ester favours the normal HWE product.

HETEROCYCLIC ANTIVIRAL COMPOUNDS

Compounds having the formula I wherein R1, R2, R3, R4, and R5 are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.

Rh-catalyzed Negishi alkyl-aryl cross-coupling leading to α- or β-phosphoryl-substituted alkylarenes

The catalytic cross-coupling between ArZnX and ICH2(CH 2)nP(O)(OEt)2 (n = 0-3) has been investigated to determine the utility of the Rh catalyst during the alkyl-aryl cross-coupling and to develop a new syntheti

The first synthesis of the epoxide-containing macrolactone nucleus of oximidine I

A synthesis of the epoxydiene-containing macrolide nucleus of oximidine I is reported, starting from commercially available 3-butyn-1-ol. The key macrocyclisation step is achieved using Horner-Wadsworth-Emmons methodology in the presence of an epoxide.

Facile Synthesis of 9,10-Dihydro-4H-Benzo [4,5] Cyclohepta [1,2-b] Thiophene-4-One: A Crucial Drug Intermediate-Application of Wittig-Horner Reaction

Synthesis of 9,10-dihydro-4H-benzo [4,5] cyclohepta[1,2-b] thiophene-4-one, a key pharmaceutical intermediate was described by two different routes. The formation of Cannizzaro reaction products was observed in first route. Wittig-Horner reaction conditions were utilized in the second route to obtain the title compound in good yield.