65118-17-4

Upstream product

• 1694-92-4 2-Nitrobenzenesulfonyl chloride 
• 107-11-9 1-amino-2-propene 
• 908072-33-3 2-nitro-N-(prop-2-yn-1-yl)benzene-1-sulfonamide 
• 198572-71-3 N-(tert-butoxycarbonyl)-2-nitrobenzenesulfonamide 

Downstream Products

• 107616-16-0 o-amino-N-2-propenylbenzenesulfonamide 
• 309248-36-0 methyl (1R,4S)-4-(N-nosyl-1-prop-2-enylamino)cyclopent-2-enyl carbonate 
• 501415-98-1 (-)-(1S,3S,5S)-5-(N-allyl-N-(2-nitrobenzenesulfonyl)amino)-3-(tert-butyl-dimethylsilanyloxy)cyclohept-6-enyl acetate 
• 1027914-27-7 Acetic acid (1R,4R)-4-[allyl-(2-nitro-benzenesulfonyl)-amino]-cyclohept-2-enyl ester 
• 945492-91-1 (S)-N¹-allyl-N²-Boc-N¹-(o-nitrobenzenesulfonyl)-5-(triisopropylsilyloxy)pentane-1,2-diamine 
• 945493-36-7 (R)-N¹-allyl-N²-Boc-N¹-(o-nitrobenzenesulfonyl)-5-(triisopropylsilyloxy)pentane-1,2-diamine 
• 309248-43-9 4-(N-nosyl-prop-2-enylamino)cyclopent-2-enol 
• 309248-47-3 (1S,4S)-N'-(4,4-diethoxybutyl)-N,N'-dinosyl-N-prop-2-enylcyclopent-4-ene-1,3-diamine 
• 309248-40-6 (1S,4R)-N'-(4,4-diethoxybutyl)-N,N'-dinosyl-N-prop-2-enylcyclopent-4-ene-1,3-diamine 
• 1018387-83-1 (Z)-N-allyl-N-[4-(2''-(benzyloxymethyl)allyloxy)but-2'-enyl]-2-nitrobenzenesulfonamide 
• 1018389-28-0 N-allyl-N-(hex-5-enyl)-2'-nitrobenzenesulfonamide 
• 1018389-35-9 (+/-)-N-allyl-N-(1-methylbut-3-enyl)-2'-nitrobenzenesulfonamide 
• 1127305-89-8 C₄₇H₅₆F₁₇N₃O₉S₂Si 
• 1127305-97-8 (Z)-N-{4'-[N''-allyl-(2-nitrobenzenesulfonamido)]-but-2'-yn-1'-yl}-N-{4-[2-((N'-3,3,4,4,5,5,6,6,7,7,8,8,9,9,10,10,10-heptadecafluorodecyl)-4-methylbenzenesulfonamido)methylallyloxy]but-2-enyl}-2-nitrobenzenesulfonamide 

Relevant academic research and scientific papers

Twofold Radical-Based Synthesis of N, C-Difunctionalized Bicyclo[1.1.1]pentanes

Bicyclo[1.1.1]pentylamines (BCPAs) are of growing importance to the pharmaceutical industry as sp3-rich bioisosteres of anilines and N-tert-butyl groups. Here we report a facile synthesis of 1,3-disubstituted BCPAs using a twofold radical functionalization strategy. Sulfonamidyl radicals, generated through fragmentation of α-iodoaziridines, undergo initial addition to [1.1.1]propellane to afford iodo-BCPAs; the newly formed C-I bond in these products is then functionalized via a silyl-mediated Giese reaction. This chemistry also translates smoothly to 1,3-disubstituted iodo-BCPs. A wide variety of radical acceptors and iodo-BCPAs are accommodated, providing straightforward access to an array of valuable aniline-like isosteres.

MACROCYCLIC COMPOUNDS AND THEIR USE IN THE TREATMENT OF DISEASE

The invention relates to heterocyclic compounds of the formula (I), in which all of the variables are as defined in the specification; capable of modulating the activity of CFTR. The invention further provides a method for manufacturing compounds of the invention, and its therapeutic uses. The invention further provides methods to their preparation, to their medical use, in particular to their use in the treatment and management of diseases or disorders including Cystic fibrosis and related disorders.

Consecutive Aminolithiation-Carbolithiation of a Linear Aminoalkene Bearing Terminal Vinyl Sulfide Moiety to Give Hydro-indolizine

Aminolithiation-carbolithiation tandem cyclization of an aminoalkene bearing vinyl sulfide moiety proceeded smoothly using stoichiometric amounts of BuLi. Both aminolithiation and carbo-lithiation were in equilibrium at room temperature, and the stereoche

DIAZABICYCLO[4.3.1]DECANE DERIVATIVES FOR TREATMENT OF PSYCHIATRIC DISORDERS

The present invention relates to diazabicyclo[4.3.1]decane derivatives, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said diazabicyclo[4.3.1]decane derivatives can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

An Enantioselective Cascade Cyclopropanation Reaction Catalyzed by Rhodium(I): Asymmetric Synthesis of Vinylcyclopropanes

N-Tosylhydrazone-yne-ene substrates are satisfactorily prepared and their cyclization under rhodium catalysis is evaluated. A cascade process involving rhodium vinyl carbene formation – through carbene/alkyne metathesis – and cyclopropanation has been dev

DIAZABICYCLO[4.3.1]DECANE DERIVATIVES FOR TREATMENT OF PSYCHIATRIC DISORDERS

The present invention relates to diazabicyclo[4.3.1 ]decane derivatives (I), pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said diazabicyclo[4.3.1]decane derivatives are specific inhibitors of the FK506 binding proteins (FKBP's) and can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Diazabicyclo[4.3.1]decane derivatives for treatment of psychiatric disorders

The present invention relates to diazabicyclo[4.3.1]decane derivatives of formula (I), pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said diazabicyclo[4.3.1]decane derivatives are inhibitors of the FK506 binding protein (FKBP's) and can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.

Chemoselective hydrogenation reaction of unsaturated bonds in the presence of an o-nitrobenzenesulfonyl group

Chemoselective hydrogenation of unsaturated compounds bearing an o-nitrobenzenesulfonyl (Ns)-amide moiety, affording the corresponding saturated compounds, was accomplished efficiently without loss of the nitro group by using the Pd/MS3A catalyst and a H2 balloon. Partial hydrogenation of alkynes bearing an Ns group to corresponding cis alkenes was achieved with the combination of the Pd/BN catalyst and an additive (diethylenetriamine or acetic acid).

Effect of added salt on ring-closing metathesis catalyzed by a water-soluble hoveyda-grubbs type complex to form N-containing heterocycles in aqueous media

The efficiency of ring-closing metathesis catalyzed by a Hoveyda-Grubbs type catalyst in water can be enhanced by addition of a chloride salt under neutral conditions. UV-vis spectroscopic study showed that a characteristic band of the catalyst around 380 nm remained over 16 h in the presence of KCl, whereas the band distinctly decreased in the absence of KCl. The disappearance of the band is ascribed to a displacement of a chloride ligand by a water molecule or a hydroxide anion. The spectral changes can be related to the metathesis activity. The experimental results indicate that avoidance of the chloride ligand loss is important to maintain the metathesis activity in water.

Regioselectivity in the intramolecular heck reaction of a series of cyclic sulfonamides: An experimental and computational study

Regioselectivity in the intramolecular Heck reaction of a series of N-sulfonyl-2,5-dihydro-3-substituted pyrroles was studied. These substrates are unbiased in terms of the formed ring size of the new heterocycle. Results indicate that high levels of regi