286956-03-4

Upstream product

• 99-91-2 para-chloroacetophenone 
• 135-02-4 ortho-anisaldehyde 

Downstream Products

• 211753-40-1 2-Amino-6-(4-chloro-phenyl)-4-(2-methoxy-phenyl)-nicotinonitrile 
• 1620583-16-5 2,3-dibromo-1-(4-chlorophenyl)-3-(2-methoxyphenyl)propan-1-one 
• 1620583-15-4 (4-chlorophenyl)(1-isopropyl-3-(2-methoxyphenyl)aziridin-2-yl)methanone 
• 1620583-14-3 ethyl 5-(4-chlorobenzoyl)-1-isopropyl-2-(2-methoxyphenyl)-1H-imidazole-4-carboxylate 
• 1620583-13-2 ethyl 5-((4-chlorophenyl)(hydroxy)methyl)-1-isopropyl-2-(2-methoxyphenyl)-1H-imidazole-4-carboxylate 
• 1620583-12-1 ethyl 5-((4-chlorophenyl)(methylsulfonyloxy)methyl)-1-isopropyl-2-(2-methoxyphenyl)-1H-imidazole-4-carboxylate 
• 1620583-11-0 ethyl 5-((3-chloro-2-fluorophenylamino)(4-chlorophenyl)methyl)-1-isopropyl-2-(2-methoxyphenyl)-1H-imidazole-4-carboxylate 
• 1620582-84-4 1-(3-chloro-2-fluoro-phenyl)-6-(4-chloro-phenyl)-7-isopropyl-8-(2-methoxy-phenyl)-1,3,6,7-tetrahydro-purin-2-one 
• 1620583-10-9 5-((3-chloro-2-fluorophenylamino)(4-chlorophenyl)methyl)-1-isopropyl-2-(2-methoxyphenyl)-1H-imidazole-4-carboxylic acid 
• 211753-25-2 4-Amino-7-(4-chloro-phenyl)-5-(2-methoxy-phenyl)-1H-pyrido[2,3-d]pyrimidine-2-thione 

Relevant academic research and scientific papers

Potent, orally absorbed glucagon receptor antagonists

The SAR of 2-pyridyl-3,5-diaryl pyrroles, ligands of the human glucagon receptor and inhibitors of p38 kinase, were investigated. This effort resulted in the identification of 2-(4-pyridyl)-5-(4-chlorophenyl)-3-(5- bromo-2-propyloxyphenyl)pyrrole 49 (L-168,049), a potent (Kb = 25 nM), selective antagonist of glucagon.

SUBSTITUTED PURINONE COMPOUNDS

The invention relates to compounds of formula (I): (I) as described herein, pharmaceutical preparations comprising such compounds, uses and methods of use for such compounds in the treatment of a disorder or a disease mediated by the activity of MDM2 and/or MDM4, and combinations comprising such compounds.

Amberlyst-15 and Amberlite-200C: Efficient catalysts for aldol and cross-aldol condensation under ultrasound irradiation

This paper presents an improved synthesis of trans-chalcones and α,α′-bis(arylmethylidene) cycloalkanones under ultrasound irradiation in the presence of commercial acid-resins as catalysts in solvent free conditions. Several trans-chalcones and α,α′- bis(arylmethylidene) cycloalkanones were synthesized in good yields and excellent selectivity in a short reaction time.

Evaluation of silica-H2SO4 as an efficient heterogeneous catalyst for the synthesis of chalcones

We report an efficient silica-H2SO4 mediated synthesis of a variety of chalcones that afforded the targeted compounds in very good yield compared to base catalyzed solvent free conditions as well as acid or base catalyzed refluxing conditions.

The ortho effect: Copper-catalyzed highly enantioselective 1,4-conjugate addition of diethylzinc to chalcones

The copper-catalyzed enantioselective 1,4-conjugate addition of diethylzinc to chalcones was investigated in the presence of a catalytic amount of N,P-ferrocenyl ligands with central and planar chirality under mild conditions (0 °C→rt). It was found that chalcones with ortho-substituents (from ortho-substituted benzaldehydes and acetophenone/substituted acetophenones) led to a dramatic improvement in the enantioselectivities. The (R)- and (S)-antipodes of the addition reaction were obtained with up to 92% ee after this transformation.

The pyrrole moiety as a template for COX-1/COX-2 inhibitors

Aroyl- and thiophene-substituted pyrrole derivatives have been synthesized as a new class of COX-1/COX-2 inhibitors. The inhibition of COX-1 was evaluated in a biological system using bovine PMNLs as the enzyme source, whereas LPS-stimulated human monocytes served as the enzyme source for inducible COX-2. The determination of the concentration of arachidonic acid metabolites was performed by HPLC for COX-1 and RIA for COX-2. Variation of the substitution pattern led to a series of active compounds which showed inhibition for COX-1 and COX-2. Structural requirements for the development of COX-1/COX-2 inhibitors are discussed. (C) 2000 Editions scientifiques et medicales Elsevier SAS.