222835-03-2

Upstream product

• 4397-53-9 p-benzyloxybenzaldehyde 
• 13676-06-7 ethyl 2-ethoxy-2-(diethylphosphono)acetate 
• 16847-90-8 (1,2-diethoxy-2-oxoethyl)triphenylphosphonium chloride 
• 100-44-7 benzyl chloride 
• 123-08-0 4-hydroxy-benzaldehyde 
• 361576-28-5 3-(4-benzyloxy-phenyl)-2-ethoxy-3-hydroxy-propionic acid ethyl ester 
• 6065-82-3 Ethyl diethoxyacetate 
• 34006-60-5 ethyl 2-chloro-2-ethoxyacetate 

Downstream Products

• 24807-40-7 methyl 3-(4-benzyloxyphenyl)propanoate 
• 222555-05-7 ethyl (2R)-2-ethoxy-3-(4-hydroxyphenyl)propanoate 
• 325793-65-5 (2S)-2-Ethoxy-3-(4-hydroxyphenyl)propanoic acid 
• 222555-06-8 ethyl (2S)-2-ethoxy-3-(4-hydroxyphenyl)propanoate 
• 1056456-02-0 (S)-2-ethoxy-3-(4-((5-(3-methoxyphenyl)-3-methylthiophen-2-yl)methoxy)phenyl)propionic acid ethyl ester 
• 1056455-43-6 (S)-2-ethoxy-3-(4-((5-(3-methoxyphenyl)-3-methylthiophen-2-yl)methoxy)phenyl)propionic acid 
• 1056456-04-2 (S)-3-(4-((5-bromo-3-methylthiophen-2-yl)methoxy)phenyl)-2-ethoxypropionic acid ethyl ester 
• 1056456-28-0 (S)-2-ethoxy-3-(4-((3-methylthiophen-2-yl)methoxy)phenyl)propionic acid ethyl ester 
• 325793-71-3 (S)-2-ethoxy-3-(4-hydroxyphenyl)propanoic acid isopropyl ester 
• 222834-30-2 ragaglitazar 
• 197299-16-4 ethyl 2-ethoxy-3-(4-hydroxy-phenyl)-propionate 
• 223126-28-1 3-(4-benzyloxyphenyl)-2-ethoxypropanoic acid ethyl ester 
• 251454-47-4 3-[4-(Benzyloxy)phenyl]-2-ethoxypropanoic acid 
• 251454-48-5 3-(4-benzyloxyphenyl)-(S)-2-ethoxy-N-(2-hydroxy-(R)-1-phenylethyl)propanoic amide 

Relevant academic research and scientific papers

PYRIMIDINYL-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PPAR AGONISTS

The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compou

NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED GAMMA RECEPTOR MODULATORS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention provides a novel phenylpropionic acid derivative and a PPAR-γ modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-γ and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.

PYRIMIDINYL-PROPIONIC ACID DERIVATIVES AND THEIR USE AS PPAR AGONISTS

The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compou

NOVEL PHENYLPROPIONIC ACID DERIVATIVES AS PEROXISOME PROLIFERATOR-ACTIVATED GAMMA RECEPTOR MODULATORS, METHOD OF THE SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME

The present invention provides a novel phenylpropionic acid derivative and a PPAR-γ modulator comprising the same as an active ingredient. The phenylpropionic acid derivative of the present invention has modulatory action on function of PPAR-γ and then exhibits hypoglycemic, hypolipidemic and insulin resistance-reducing effects on PPAR-mediated diseases or disorders. Therefore, the present invention is prophylactically or therapeutically effective for diabetes and metabolic diseases.

Design, synthesis, and structure-activity relationship of carbamate-tethered aryl propanoic acids as novel PPARα/γ dual agonists

We have developed a new class of PPARα/γ dual agonists, which show excellent agonistic activity in PPARα/γ transactivation assay. In particular, (R)-9d was identified as a potent PPARα/γ dual agonist with EC50s of 0.377 μM in PPARα and 0.136 μM in PPARγ, respectively. Interestingly, the structure-activity relationship revealed that the stereochemistry of the identified PPARα/γ dual agonists significantly affects their agonistic activities in PPARα than in PPARγ.

Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor α/γ agonist ragaglitazar

A new and improved synthesis of the peroxisome proliferator-activated receptor (PPAR) agonist ragaglitazar applicable for large-scale preparation has been developed. The convergent synthetic procedure was based on a novel enzymatic kinetic resolution step

Process development on the enantioselective enzymatic hydrolysis of S-ethyl 2-ethoxy-3-(4-hydroxyphenyl)propanoate

A novel biocatalytic approach for the large-scale production of S-2-ethoxy-3-(4-hydroxyphenyl)propanoic acid S-1 from its racemic ethylester rac-2 by enantioselective hydrolysis has been developed. S-1 is an important building block in the synthesis of PPARα and -γ agonists such as Ragaglitazar [NNC 61-0029 ((-)DRF2725)]. The development history comprises enzyme screening, biocatalyst and process optimization, and scale-up to pilot plant. The project was thereby highly interdisciplinary by combining biotechnology and chemistry technologies. The final process was successfully run on a 44-kg pilot scale in 43-48% yields and with high enantiomeric purities (98.4-99.6% ee).

AMIDE LINKER PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR MODULATORS

The present invention is directed to compounds, compositions, and use of compounds the structural Formula (I).

3-aryl-2-hydroxypropionic acid derivative III

A novel 3-aryl-2-hydroxypropionic acid derivative, a process and intermediate for its manufacture, pharmaceutical prepartions containing it and the use of the compound in clinical conditions associated with insulin resistance.