193635-17-5

Upstream product

• 98-59-9 p-toluenesulfonyl chloride 
• 62456-75-1 N-[(4-methylphenyl)sulfonyl]-β-alanine methyl ester 
• 6638-79-5 N,O-dimethylhydroxylamine*hydrochloride 
• 42908-33-8 3-{[(4-methylphenyl)sulfonyl]amino}propanoic acid 
• 1117-97-1 N,0-dimethylhydroxylamine 
• 107-95-9 3-amino propanoic acid 
• 193634-77-4 N-methoxy-N-methylacrylamide 
• 55962-05-5 [N-(p-tolylsulfonyl)imino]phenyliodinane 
• 193634-86-5 N-methoxy-N-methyl-1-(p-toluenesulfonyl)aziridine-2-carboxamide 

Downstream Products

• 1424888-75-4 C₂₅H₃₈N₂O₅SSi 
• 1424888-77-6 C₂₅H₃₈N₂O₅SSi 

Relevant academic research and scientific papers

Ring Expansion Fluorination of Unactivated Cyclopropanes Mediated by a New Monofluoroiodane(III) Reagent

Herein, we report a new strategy for carbon?carbon bond scission and intramolecular ring expansion fluorination of unactivated cyclopropanes, which was accomplished with a new hypervalent fluoroiodane(III) reagent 1. This novel method delivers medicinally relevant 4-fully substituted fluoropiperidines in moderate to high yields with excellent regio- and diastereoselectivity. Reagent 1, which has an N-acetylbenziodazole framework, was readily synthesized via three steps in 76 % overall yield and was characterized by NMR spectroscopy and X-ray crystallography. Owing to the presence of a secondary I???O bonding interaction between the λ3-iodane atom and the carbonyl oxygen of the acetyl group of the N-acetylbenziodazole framework, 1 has excellent stability and can be stored at ambient temperature for 6 months without any detectable decomposition. Density functional theory calculations and experimental studies showed that the reaction proceeds via a carbocation intermediate that readily combines with a fluoride ion to generate the product.

NRF2 REGULATORS

Provided are aryl analogs，pharmaceutical compositions containing them and their use as NRF2 regulators.

Gold(I)/copper(II)-cocatalyzed tandem cyclization/semipinacol reaction: Construction of 6-Aza/Oxa-Spiro[4.5]decane skeletons and formal synthesis of (±)-halichlorine

A simple and efficient strategy for the construction of 6-aza/oxa-spiro[4.5]decane skeletons under the cocatalysis of gold(I)/copper(II) was developed, and its potential utility was demonstrated by a formal synthesis of the biologically active marine alkaloid (±)-halichlorine.

A novel method for synthesizing 3-arylpyrrolidine and 4-arylpiperidine derivatives through an acid-promoted skeletal rearrangement

A novel method for synthesizing 3-arylpyrrolidine and 4-arylpiperidine derivatives through an acid-promoted skeletal rearrangement is described. Using trifluoroacetic acid as the acid promoter, an intramolecular ipso-Friedel-Crafts-type addition of phenols to allyl cations, formation of iminium cations through rearomatization of the spirocyclohexadienone units, and an intramolecular aza-Prins reaction, proceeded sequentially to afford 3-arylpyrrolidine and 4-arylpiperidine derivatives in good yield with high diastereoselectivity.

Reduction of 2-acylaziridines by samarium(II) iodide. An efficient and regioselective route to β-amino carbonyl compounds

A convenient method for the reduction of 2-acylaziridines, aziridine-2- carboxylates and aziridine-2-carboxamides is described. The reduction of all of the substrates examined was extremely rapid and highly regioselective, giving rise to β-amino carbonyl compounds. This method appears to be general for all of the classes of aziridines mentioned above, and also tolerates a variety of nitrogen protecting groups.