477585-31-2

Upstream product

• 477585-26-5 sodium 4-(2-methylquinolin-4-ylmethoxy)benzenesulfonate 
• 825-90-1 sodium p-hydroxybenzenesulfonate 
• 91-56-5 indole-2,3-dione 
• 4939-28-0 4-(hydroxymethyl)-2-methylquinoline 
• 634-38-8 2-methylquinoline-4-carboxylic acid 
• 477585-25-4 4-(2-methylquinolin-4-ylmethyloxy)thiophenol disulphide 

Downstream Products

• 675185-11-2 [1-({4-[(2-methylquinolin-4-yl)methoxy]phenyl}sulphonyl)pyrrolidin-2-yl]methanol 
• 910332-21-7 4-[4-(2-methyl-quinolin-4-ylmethoxy)-benzenesulfonylamino]-tetrahydro-pyrane-3-carboxylic acid methyl ester 
• 910332-37-5 4-[4-(2-methyl-quinolin-4-ylmethoxy)-benzenesulfonylamino]-piperidine-1,3-dicarboxylic acid 1-tert-butyl ester 3-methyl ester 
• 910332-55-7 3-[4-(2-methyl-quinolin-4-ylmethoxy)-benzenesulfonylamino]-piperidine-1,4-dicarboxylic acid 1-tert-butyl ester 4-ethyl ester 
• 910333-05-0 1-tert-butyl 3-methyl (3R,4R)-3-hydroxy-4-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}sulfonyl)amino]piperidine-1,3-dicarboxylate 
• 910333-41-4 methyl (1R,2R)-1-hydroxy-2-[({4-[(2-methylquinolin-4-yl)methoxy]phenyl}sulfonyl)amino]cyclopentanecarboxylate 
• 675185-23-6 (5R)-5-methyl-5-[(2R)-1-({4-[(2-methylquinolin-4-yl)methoxy]phenyl}sulphonyl)pyrrolidin-2-yl]imidazoline-2,4-dione 
• 1260171-61-6 (S)-N-hydroxy-2-(4-isobutyrylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]propionamide 
• 1260171-67-2 (S)-N-allyloxy-2-(4-isobutyrylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]propionamide 
• 1260171-71-8 methyl (S)-2-[4-(2-methylpropane-1-sulfonyl)piperazin-1-yl]-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]propanoate 
• 910331-90-7 (1S,2R)-2-[4-(2-methylquinolin-4-ylmethoxyl)benzenesulfonylamino]cyclopentane carboxylic acid 
• 1260171-34-3 methyl (S)-2-(4-benzylpiperazin-1-yl)-3-[4-(2-methylquinolin-4-ylmethoxy)benzenesulfonylamino]propanoate 

Relevant academic research and scientific papers

NOVEL BENZENESULFONAMIDE COMPOUNDS, METHOD FOR SYNTHESIZING SAME, AND USE THEREOF IN MEDICINE AS WELL AS IN COSMETICS

Provided herein are novel benzenesulfonamide compounds having a structure of formula (I) below: as well as to the method for synthesizing same and to the use thereof in pharmaceutical compositions to be used in human or veterinary medicine, as well as to

Development of a suitable process for the preparation of a TNF-α converting enzyme inhibitor, WAY-281418

A suitable process for the preparation of kilogram quantities of a TNF-α converting enzyme (TACE) inhibitor (WAY-281418) was developed using isatin 13 as starting material and an efficient coupling step for the formation of sulfonamide 8 in a 15% overall yield. Process preparation of (+)-(1S,2R)-2-aminocyclopentane-1-carboxylic acid (7, (+)-cispentacin), a chiral component for WAY-281418, was successfully scaled up via an asymmetric hydroge-nation reaction. Crystallization allowed the isolation of all intermediates and the final product 9.

SULPHONAMIDE DERIVATIVES AND THEIR USE AS TACE INHIBITORS

Sulphonamide derivatives that are useful in the inhibition of metalloproteinases and in particular in the inhibition of TNF-α Converting Enzyme (TACE).