210691-47-7

Upstream product

• 30414-53-0 methyl propanoyl acetate 
• 100-39-0 benzyl bromide 
• 100-44-7 benzyl chloride 
• 591-50-4 iodobenzene 
• 133181-02-9 3-hydroxy-2-methylene-pentanoic acid methyl ester 
• 108-86-1 bromobenzene 

Downstream Products

• 434899-25-9 C₁₄H₁₆O₄ 
• 79141-05-2 1-phenyl-2-methylidenopentan-3-one 
• 23936-95-0 (2R)-2-methyl-1-phenyl-3-pentanone 
• 1443147-50-9 4-benzyl-3-ethyl-1-phenyl-1,4-dihydro-5H-pyrazol-5-one 
• 1264295-39-7 methyl 2-methyl-2-(3-methyl-8-(4-(trifluoromethyl)phenyl)pyrazolo[5,1-c][1,2,4]triazin-4-yl)-3-phenylpropanoate 
• 1264296-41-4 methyl 2-benzyl-4-(diethoxyphosphoryl)-2-methyl-3-oxopentanoate 
• 1264296-40-3 methyl 2-benzyl-4-bromo-2-methyl-3-oxopentanoate 
• 1264296-39-0 methyl 2-benzyl-2-methyl-3-oxopentanoate 
• 863400-52-6 6-benzyl-2-tert-butyl-7-ethyl-5-hydroxy-[1,2,4]triazolo[1,5-a]pyridine-8-carbonitrile 
• 677723-00-1 4-acetylsulfanyl-2-benzyl-3-oxo-pentanoic acid methyl ester 
• 677722-94-0 3-benzyl-4-hydroxy-5-methyl-5H-thiophen-2-one 

Relevant academic research and scientific papers

Palladium catalysed reactions of Baylis-Hillman products: Synthesis of some useful intermediates

Acetates derived from Baylis-Hillman products were reacted with sodio dimethyl (or diethyl) malonate under Pd(O) catalysis to form E olefins as the major products. Likewise, the Heck reaction with these acetates as well as with the corresponding alcohols

Design, Synthesis, and Structure-Activity Relationship Study of Pyrazolones as Potent Inhibitors of Pancreatic Lipase

Pancreatic lipase (PL), a key target for the prevention and treatment of obesity, plays crucial roles in the hydrolysis and absorption of in dietary fat. In this study, a series of pyrazolones was synthesized, and their inhibitory effects against PL were

Discovery of pyrazolones as novel carboxylesterase 2 inhibitors that potently inhibit the adipogenesis in cells

Carboxylesterase 2 (CES2) is one of the most important Phase I drug metabolizing enzymes in the carboxylesterase family. It plays crucial roles in the bioavailability of oral ester prodrugs and the therapeutic effect of some anticancer drugs such as irino

Bioreduction of α-Acetoxymethyl Enones: Proposal for an SN2′ Mechanism Catalyzed by Enereductase

(Z)-3-Acetoxymethyl-4-R-3-buten-2-ones (R=aryl, alkyl) and (Z)-3-methyl-4-R-3-buten-2-ones (R=aryl) were synthesized and submitted to reduction by the yeast Saccharomyces cerevisiae producing the (R)- and (S)-4-R-3-methybutan-2-ones, respectively. This stereochemistry control strategy was applied in the syntheses of (R)- and (S)-Tropional with moderate to high enantiomeric excesses. Other (Z)-3-acyloxymethyl-4-phenyl-3-buten-2-ones showed similar behavior to the (Z)-3-acetoxymethyl counterpart, and the acylated Morita–Baylis–Hillman adduct 1-acetoxy-2-methylene-1-phenylbutan-3-one produced a mixture of products, with and without the acetoxy group, via three different reaction pathways. In addition to experiments employing whole cells, those in which isolated enereductases were used suggested that the main pathway through which the loss of the acetoxy group occurs during the biocatalytic cascade is an SN2′-type reaction, rather than formal hydrogen addition followed by acetic acid elimination. Finally, related ethyl enones were reduced enantioselectively by the yeast Candida albicans, producing both (R)- and (S)-reduction products, depending on the presence of the acetoxy group in the starting material. (Figure presented.).

COMPOUNDS AND COMPOSITIONS AS MODULATORS OF GPR119 ACTIVITY

The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.

FUNGICIDAL HETEROCYCLIC COMPOUNDS

A compound which can specifically or selectively expresses an antifungal activity with a broad spectrum, based on the functional mechanism of 1,6-β-glucan synthesis inhibition, is provided, and an antifungal agent which comprises such a compound, a salt thereof or a solvate thereof is provided. A compound represented by the following formula (I), a salt thereof or a solvate thereof.

Propanoic acid derivatives that inhibit the binding of integrins to their receptors

A compound of the structure A method for the inhibition of the binding of α4β1integrin to its receptors, for example VCAM-1(vascular cell adhesion molecule-1) and fibronectin; pharmaceutically active compositions comprising these compounds; and the use of these compounds for the control or prevention of diseases states in which α4β1is involved are also disclosed.

Analogues of thiolactomycin as potential anti-malarial and anti-trypanosomal agents

A series of analogues of the naturally occurring antibiotic thiolactomycin (TLM) have been synthesised and evaluated for their ability to inhibit the growth of the malaria parasite, Plasmodium falciparum. Thiolactomycin is an inhibitor of Type II fatty acid synthase which is found in plants and most prokaryotes, but not an inhibitor of Type I fatty acid synthase in mammals. A number of the analogues showed inhibition equal to or greater than TLM. The introduction of hydrophobic alkyl groups at the C3 and C5 positions of the thiolactone ring lead to increased inhibition, the best showing a fourteenfold increase in activity over TLM. In addition, some of the analogues showed activity when assayed against the parasitic protozoa, Trypanosoma cruzi and Trypanosoma brucei.

Propanoic acid derivatives that inhibit the binding of integrins to their receptors

A method for the inhibition of the binding of α4β1 integrin to its receptors, for example VCAM-1 (vascular cell adhesion molecule-1) and fibronectin; compounds (I) that inhibit this binding; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of diseases states in which α4β1 is involved. All substituents are as defined in the application.

Facile synthesis of 1, 3-diaryl-propanones through heck reaction

1,3-diaryl propanones (1a-6a) and 1,3-diaryl-2-carbomethoxypropanones (1b-6b) have been synthesized through facile palladium catalysed arylation of Baylis-Hillman adducts.