1716-77-4

Upstream product

• 434-45-7 2,2,2-Trifluoroacetophenone 
• 7732-18-5 water 
• 63741-25-3 α-(p-tolylsulfinyl) β-hydroxy β-phenyl β-trifluoromethyl propanoate de t-butyle 
• 153816-97-8 3-phenyl-3-trifluoromethyl-3-propanolide 
• 64-19-7 acetic acid 
• 63741-28-6 R-β-hydroxy β-phenyl β-trifluoro-propanoate de t-butyle 
• 141-82-2 malonic acid 

Downstream Products

• 153816-97-8 3-phenyl-3-trifluoromethyl-3-propanolide 

Relevant academic research and scientific papers

Boron-catalyzed carboxylic acid-selective aldol reaction with trifluoromethyl ketones

A catalytic carboxylic acid-selective aldol reaction with trifluoromethyl ketones was developed. Reversible and selective covalent bond formation between a boron catalyst and a carboxylic acid is key to realizing the unprecedented catalytic aldol reaction of simple carboxylic acids. The reaction proceeded chemoselectively at the α-position of carboxylic acid even in the presence of ketone, ester, or amide functional groups in the donor substrates. The chemoselectivity is beneficial for late-stage derivatizations of biologically relevant compounds, as demonstrated by the conversion of indomethacin and triacetylcholic acid.

4-nitryl isoxazole trifluoromethyl tertiary alcohol containing compound and preparation method thereof

The invention relates to a 4-nitryl isoxazole trifluoromethyl tertiary alcohol containing compound and a preparation method thereof, and belongs to the technical field of synthesis of organic fluorine compounds. The general formula I of the compound is shown in the specification. The preparation method of the formula I comprises the steps that 3-substituent-4-nitryl-5-methyl isoxazole, trifluoromethyl aryl ketone, a catalyst and a solvent are mixed and are stirred and react at room temperature, after reacting is finished, washing, extracting, separation and purifying are carried out, and the target product 4-nitryl isoxazole trifluoromethyl tertiary alcohol containing compound is obtained. The 4-nitryl isoxazole trifluoromethyl tertiary alcohol containing compound is a series of important trifluoromethyl synthesized cut blocks, and can be used for preparing a series of novel-structure trifluoromethyl group containing organofluorine compounds such as trifluoromethylated beta-hydroxy carboxylic acid compounds and trifluoromethylated alkenyl nitryl isoxazole compounds, the yield is high, and few by-products are generated.

Piperidine derivatives with PAF antagonist activity

Compounds of general formula I and their salts and solvates are PAF antagonists and as such are useful in the treatment of various diseases or disorders mediated by PAF. Pharmaceutical compositions including these compounds and processes for their prepara

Synthesis and Structure-Activity Relationships of 1-Acyl-4-(2-methyl-3-pyridyl)cyanomethyl)piperazines as PAF Antagonists

A second generation of (cyanomethyl)piperazines, 1-acyl-4-((2-methyl-3-pyridyl)cyanomethyl)piperazines, with increased oral activity was prepared and evaluated in vitro in PAF-induced platelet aggregation assay (PAG) and in vivo in a PAF-induced hypotension test in normotensive rats (HYP).Oral activity was ascertained through a PAF-induced mortality test in mice (MOR).Attachment of a methyl group at position 2 of our earlier pyridine derivatives resulted in an improvement of 1 order of magnitude or greater in the ID50 of the oral test.Three different types of acylsubstituents of similar potency emerge from this work: N-(diphenylmethylamino)acetyl, 3-substituted 3-hydroxy-3-phenylpropionyl, and N-substituted 3-amino-3-phenylpropionyl groups.The most interesting compounds, 26 (UR-12460, PAG IC50 = 0.040 μM, HYP, ID50 = 0.021 mg/kg iv, MOR, ID50 = 0.30 mg/kg po) and 58 (UR-12519, PAG IC50 = 0.041 μM, HYP, ID50 = 0.015 mg/kg iv, MOR, ID50 = 0.044 mg/kg po), compare favorably with WEB-2086.Compounds 26 and 58 were also tested in active anaphylactic shock (AAS) and endotoxin-induced mortality (EIM) tests.On the basis of these data, compounds 26 and 58 have been selected for further pharmacological development.

CONDENSATION OF POLYFLUOROALKYL PHENYL KETONES WITH ALKYL ACETATES

A series of β-polyfluoroalkyl-β-hydroxy esters were synthesized by the condensation of polyfluoroalkyl phenyl ketones with alkyl acetates in the presence of diethylaminomagnesium bromide, and some of their transformations with thionyl chloride were studied.

FLUORINE-CONTAINING BENZALDEHYDES IN THE LEUCKART AND RODIONOV REACTIONS

Benzaldehydes containing polyfluoroalkoxy groups in the aromatic ring give the respective N-formylbenzamines by the action of formamide under the conditions of the Leuckart reaction.The products are converted by hydrolysis into benzylamines, while reducti

SYNTHESES ASYMETRIQUES DE β-HYDROXYACIDES PAR CONDENSATION D'ANIONS ENOLATES D'ESTERS α-SULFINYLE CHIRAUX SUR DES COMPOSES CARBONYLES

A stereospecific synthesis of (R)-(+)-t-butyl p-tolylsulfinyl acetate 2 is described.The aldol-type condensation of this reagent leads to β-hydroxyacids in good chemical and optical yields.The determination of the absolute configuration of the condensatio