85293-41-0

Upstream product

• 50614-39-6 2-Hydroxy-3-(4-trifluormethylbenzoyl)-propionsaeure 
• 709-63-7 1-(4-trifluoromethylphenyl)ethanone 
• 6000-59-5 glyoxalic acid monohydrate 
• 383-53-9 2-bromo-1-[4-(trifluoromethyl)phenyl]ethanone 
• 56893-13-1 (2-oxo-2-(4-(trifluoromethyl)phenyl)ethyl)triphenylphosphonium bromide 
• 298-12-4 Glyoxilic acid 

Downstream Products

• 1579957-74-6 C₁₃H₁₁F₃O₄ 
• 1579957-55-3 (3R,3'R,5'R)-1-methyl-3'-(2-oxo-2-(4-(trifluoromethyl)phenyl)ethyl)-5'-(2-oxo-2-phenylethyl)-5',6'-dihydrospiro[indoline-3,4'-pyran]-2,2'(3'H)-dione 
• 1579957-31-5 (E)-(E)-4-oxo-4-phenylbut-2-en-1-yl4-oxo-4-(4-(trifluoromethyl)phenyl)but-2-enoate 
• 1579957-88-2 C₁₃H₉F₃O₄ 
• 53498-75-2 2-(trifluoromethyl)-6-(4-(trifluoromethyl)phenyl)isonicotinic acid 

Relevant academic research and scientific papers

Enantiopure substituted pyridines as promising antimalarial drug candidates

We describe the enantioselective synthesis and biological evaluation of 4-(2-amino-1-hydroxyethyl)pyridines (4 AHPs) as new antimalarial drug candidates. In particular, two routes to obtain the key-intermediate 4-vinyl-pyridine were studied. These routes are based on a Kr?hnke-type cyclization or on metal-catalyzed reactions. The Kr?hnke-type cyclization route is faster but only efficient at low scale since this pathway involves a Wittig reaction that requires severe temperature-control. Consequently, we designed a second route based on metal-catalyzed reactions. This way is longer but the 4-vinyl-pyridine can be obtained on a 5 g scale at least. Finally, a regioselective SN2 ring-opening of enantiopure epoxides by alkyl primary amines allowed the synthesis of eight 4-AHPs with global yields up to 41%. These compounds show strong in vitro antimalarial activity against P. falciparum strains and are more active that chloroquine and mefloquine. These results demonstrate that 4-AHPs are promising antimalarial drug candidates.

Hydrogen-bond-directed formal [5 + 1] annulations of oxindoles with ester-linked bisenones: Facile access to chiral spirooxindole δ-lactones

A novel bifunctional thiourea catalyzed formal [5 + 1] cycloaddition of oxindoles and ester-linked bisenones was successfully developed. This strategy involves two sequential Michael additions, leading to spirooxindole δ-lactones with three contiguous ste

Arylalkane, arylalkene and aryl azaalkane, medicaments containing said compounds and method for the production thereof

The present invention relates to compounds of general formula [in-line-formulae]R—Z1—Z2—Z3—R1, ??(I)[/in-line-formulae] wherein R, R1 and Z1 to Z3 are defined as in claim 1, the tautomers, the diastereomers, the enantiomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly CGRP-antagonistic properties, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Gastric anti-secretory, anti-ulcer and cytoprotective properties of substituted (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids

A class of anti-secretory, anti-ulcer and cytoprotective agents, the substituted (E)-4-phenyl and heteroaryl-4-oxo-2-butenoic acids, is described.This chemical structure is not related to those of any known anti-cholinergic drugs, histamine H2-receptor antagonists or prostaglandins.Five compounds, 4-(2-methoxyphenyl)- 15, 4-(4-methoxyphenyl)- 22, 4-(3,4-dimethoxyphenyl)- 32, 4-(3,4,5-trimethoxyphenyl)- 40, and 4-(2-furanyl)-4-oxo-2-butenoic acid 44, have cytoprotective activity at a very low dose (0.6 mg/kg, p.o.) and anti-secretory and anti-ulcer activities at higher doses.One of these compounds, RU 38086 40, has been selected for clinical evaluation.Keywords - anti-ulcer agents / cytoprotective agents / (E)-4-phenyl- and heteroaryl-4-oxo-2-butenoic acids.

Gastro-protecting activity

Diseases and ailments accompanied by gastric and gastroduodenal lesions treated by administering a compound of the formula (I) STR1 in which R represents hydrogen or alkyl containing 1 to 5 carbon atoms and R1 and R2, identical or different, both represent alkoxy containing 1 to 3 carbon atoms, or both represent halogen, or R1 represents hydrogen and R2 represents halogen, nitro or trifluoromethyl, or R1 and R2 form a methylenedioxy group at adjacent carbon atoms, as well as pharmaceutically acceptable salts thereof, particularly alkali metal, alkaline earth metal, or amine salts of said acid.