800384-35-4

Upstream product

• 98-68-0 4-methoxy-phenyl-sulphonyl chloride 
• 2450-71-7 Propargylamine 
• 55125-01-4 N-(t-butoxycarboyl)-4-methoxyphenylsulfonamide 

Downstream Products

• 1147121-52-5 N-(3,3-dimethylallyl)-4-methoxyl-N-(prop-2-ynyl)benzenesulfonamide 

Relevant academic research and scientific papers

Ruthenium Carbene-Mediated Construction of Strained Allenes via the Enyne Cross-Metathesis/Cyclopropanation of 1,6-Enynes

Herein, we report on the unprecedented dimerization of 1,6-enynes using a commercially available ruthenium complex RuCl2(PPh3)3, which results in a series of bicyclo[3.1.0]hexyl allene derivatives in moderate to excellent yields. Mechanistic investigation indicates that the in-situ-generated ruthenium vinylidene undergoes a site-selective metathesis process to provide allenyl ruthenium carbene, which can be intramolecularly trapped by the pendent C=C bond of enyne through a [2 + 2] cycloaddition/metal elimination process.

BTK Inhibitors and uses thereof

The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.

Structure optimization and bioactivity evaluation of ThDP analogs targeting cyanobacterial pyruvate dehydrogenase E1

Harmful cyanobacteria bloom (HCB) has occurred frequently in recent years and it is urgent to develop novel algicides to deal with this problem. In this paper, a series of novel thiamin diphosphate (ThDP) analogs 5a?5g were designed and synthesized target

Enantioselective Synthesis of All-Carbon Quaternary Centers Structurally Related to Amaryllidaceae Alkaloids

Enantioselective synthesis of all-carbon quaternary centers remains a considerable challenge for synthetic organic chemists. Here, we report a two-step protocol to synthesize such centers including tandem cyclization/Suzuki cross-coupling followed by halocarbocyclization. During this process, two rings, three new C?C bonds and a stereochemically defined all-carbon quaternary center are formed. The absolute configuration of this center is controlled by the stereochemistry of the adjacent stereocenter, which derives from an appropriate enantioenriched starting material. Using this method, we synthesized polycyclic compounds structurally similar to Amaryllidaceae alkaloids in high enantiomeric excesses. Because these products resemble naturally occurring compounds, our protocol can be used to synthesize various potentially bioactive compounds.

Substrate Control in the Gold(I)-Catalyzed Cyclization of β-Propargylamino Acrylic Esters and Further Transformations of the Resultant Dihydropyridines

N-Protected β-propargylamino acrylic esters with a push-pull olefinic bond afforded good to high yields of dihydropyridines upon treatment with 5% tris(2-furyl)phosphine-gold(I) chloride/silver(I) tetrafluoroborate [(TFP)AuCl/AgBF4] in anhydrous benzene. Carbamate and sulfonyl groups were employed for nitrogen protection. On a model enyne, the p-methoxybenzenesulfonyl (MBS) group was found to be a better protective group than tosyl in terms of cyclization yield, and also the yield of elimination to the corresponding 2,3,4-trisubstituted pyridines. Boc-protected dihydropyridines underwent partial deprotection/oxidation under the cyclization conditions, which enabled a more straightforward, one-pot preparation of the corresponding pyridines. In another application, an appropriately substituted derivative protected as a stable methoxycarbamate was subjected to catalytic hydrogenation affording the known precursor of paroxetine. The chemoselectivity of enyne cyclization (dihydropyridine vs. pyrrole) is governed, among other factors, by C-3 substitution. Dihydropyridines were obtained as sole products regardless of the catalyst/conditions when C-3 was unsubstituted. (Figure presented.).

Design, synthesis, biological evaluation and molecular docking of amide and sulfamide derivatives as Escherichia coli pyruvate dehydrogenase complex E1 inhibitors

In this study, a series of novel amide derivatives and sulfamide derivatives as potential E. coli PDHc E1 inhibitors were designed and synthesized by optimizing the linker between triazole and benzene ring moieties based on the structure of lead compound

Regio- and chemoselective n-1 acylation of indoles: Pd-catalyzed domino cyclization to afford 1,2-fused tricyclic indole scaffolds

A concise method for the synthesis of 1,2-fused tricyclic indole scaffolds by domino cyclization involving a Pd-catalyzed Sonogashira coupling, indole cyclization, regio- and chemoselective N-1 acylation, and 1,4-Michael addition is reported. This method

Metal-free reductive cyclization and isomerization of sulfanyl-1,6-diynes using sodium borohydride

In this study, we demonstrated the metal-free reductive cyclization of sulfanyl-1,6-diynes with sodium borohydride in ethanol in the presence of diazabicyclo[5.4.0]undec-7-ene. 1,6-Diynes 1 and 5a-5h bearing hydrogen or phenyl as the R2 group a

Synthesis of trisubstituted pyrroles from rhodium-catalyzed alkyne head-to-tail dimerization and subsequent goldcatalyzed cyclization

Dimerization of N-protected propargylic amines in a rather rare head-to-tail mode has been achieved under mild conditions with high selectivity using rhodium catalysts. The JV-protecting group could be a sulfonyl, carbamate, or carbonyl functionality and

2-Phenylsulfopyrroles

The invention relates to novel 2-phenylsulfopyrroles of formula (I) wherein R1 represents lower alkyl, halo-lower alkyl, cycloalkyl, hydroxy, lower alkoxy, halo-lower alkoxy, cycloalkoxy or cyano, R2 represents hydrogen, halogen, low