70347-05-6

Upstream product

• 4919-37-3 3,5-dimethyl-4-hydroxybenzoic acid 
• 74-88-4 methyl iodide 
• 152775-45-6 4-methoxy-3,5-dimethylbenzonitrile 
• 67-56-1 methanol 
• 21553-46-8 4-methoxy-3,5-dimethylbenzoic acid 

Downstream Products

• 1350825-70-5 N'-(4-methoxy-3,5-dimethylbenzoyl)-1-methyl-5-phenyl-1H-pyrazole-3-carbohydrazide 
• 1350825-71-6 2-(4-methoxy-3,5-dimethylphenyl)-5-(1-methyl-5-phenyl-1H-pyrazol-3-yl)-1,3,4-oxadiazole 
• 1350825-72-7 2,6-dimethyl-4-(5-(1-methyl-5-phenyl-1H-pyrazol-3-yl)-1,3,4-oxadiazol-2-yl)phenol 
• 1439387-89-9 C₁₇H₁₅FN₂O₄S 
• 1422570-06-6 3-(5-(4-hydroxy-3,5-dimethylphenyl)-1,3,4-oxadiazol-2-yl)benzene-1-sulfonyl fluoride 
• 73576-38-2 α-(methylsulfonyl)-4-methoxy-3,5-dimethylacetophenone 

Relevant academic research and scientific papers

Aromatic sulfonyl fluorides covalently kinetically stabilize transthyretin to prevent amyloidogenesis while affording a fluorescent conjugate

Molecules that bind selectively to a given protein and then undergo a rapid chemoselective reaction to form a covalent conjugate have utility in drug development. Herein a library of 1,3,4-oxadiazoles substituted at the 2 position with an aryl sulfonyl fluoride and at the 5 position with a substituted aryl known to have high affinity for the inner thyroxine binding subsite of transthyretin (TTR) was conceived of by structure-based design principles and was chemically synthesized. When bound in the thyroxine binding site, most of the aryl sulfonyl fluorides react rapidly and chemoselectively with the pK a-perturbed K15 residue, kinetically stabilizing TTR and thus preventing amyloid fibril formation, known to cause polyneuropathy. Conjugation t50s range from 1 to 4 min, ～1400 times faster than the hydrolysis reaction outside the thyroxine binding site. X-ray crystallography confirms the anticipated binding orientation and sheds light on the sulfonyl fluoride activation leading to the sulfonamide linkage to TTR. A few of the aryl sulfonyl fluorides efficiently form conjugates with TTR in plasma. Eleven of the TTR covalent kinetic stabilizers synthesized exhibit fluorescence upon conjugation and therefore could have imaging applications as a consequence of the environment sensitive fluorescence of the chromophore.

PYRAZOLE DERIVATIVES AS S1P1 AGONISTS

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by sphingosine-1-phosphate receptors (S1P1) agonists.

New pyrazole derivatives

The present invention relates to a compound of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by sphingosine-1-phosphate receptors (S1P1) agonists.

OPTICALLY ACTIVE QUATERNARY AMMONIUM SALT HAVING AXIAL ASYMMETRY AND PROCESS FOR PRODUCING -AMINO ACID AND DERIVATIVE THEREOF WITH THE SAME

The present invention provides a chiral phase-transfer catalyst of the following formula (I): The compound (I) can be produced by reacting a 2,2'-dimethylene bromide-1,1'-biphenyl derivative, which can be produced through comparatively small number of steps, with an easily available secondary amine.