1370529-71-7

Upstream product

• 84459-33-6 2-bromo-4-chlorobenzaldehyde 
• 7486-35-3 tri-n-butyl(vinyl)tin 

Downstream Products

• 618891-97-7 2-ethyl-4-chlorobenzoic acid chloride 

Relevant academic research and scientific papers

AgOTf-catalyzed sequential synthesis of 4-isoquinolones: Via oxidative ring opening of aziridines and aza-Michael addition

An efficient AgOTf-catalyzed sequential reaction involving the oxidative ring-opening of aziridines by DMSO and aza-Michael addition has been developed. A series of 2,3-dihydro-4(1H)-isoquinolones were afforded in moderate to good yields by the formation of one new CO bond and one new C-N bond. The features of this sequential reaction include high bonding efficiency, use of a catalytic amount of catalysts, a broad substrate scope and mild conditions. This methodology provides a good choice for constructing the libraries of 2,3-dihydro-4(1H)-isoquinolones.

Palladium-Catalyzed Tandem Hydrocarbonylative Lactamization and Cycloaddition Reaction for the Construction of Bridged Polycyclic Lactams

The intramolecular hydroaminocarbonylation of alkenes is a compelling tool to rapidly access lactam, a privileged motif ubiquitous in natural products, pharmaceuticals, and agrochemicals. However, selective carbonylation to bridged polycyclic lactams with a lactam nitrogen at a bridgehead position is less explored. We herein report a modular palladium-catalyzed approach to perform a tandem hydrocarbonylative lactamization/Diels-Alder cycloaddition reaction with 2-vinyl aryl aldimines, alkenes, and CO, which offers convenient access to furnish the bridged polycyclic lactams in high yields with high selectivities.

Copper(I)-Catalyzed Enyne Oxidation/Cyclopropanation: Divergent and Enantioselective Synthesis of Cyclopropanes

An efficient copper(I)-catalyzed enyne oxidation/cyclopropanation for the modular synthesis of cyclopropane derivatives is described, which represents the first non-noble metal-catalyzed enynes oxidation/cyclopropanation by the in situ generated α-oxo copper carbenes. This protocol allows the assembly of valuable cyclopropane-γ-lactams in generally good to excellent yields with excellent diastereoselectivity. More significantly, the enantioselective version of enyne oxidation/cyclopropanation has been disclosed with chiral copper catalysts.

Enantioselective Remote C(sp3)-H Cyanation via Dual Photoredox and Copper Catalysis

The remote C(sp3)-H cyanation of carboxamides has been described by merging photoredox and copper catalysis in a site-selective and enantiocontrolled manner. The protocol is the integration of photoinduced and nitrogen-centered radical-mediated intermolecular hydrogen atom transfer with chiral copper-complex-catalyzed radical cyanation. This strategy gives enantio-enriched cyanated amides in high yields.

Enantioselective Copper-Catalyzed Desymmetrization of 1,3-Diketones Involving Borylation of Styrenes

A copper-catalyzed intramolecular enantioselective and diastereoselective borylative coupling of styrenes and ketones was achieved by merging desymmetrization strategy and olefin difunctionalization. The reaction proceeds through an initial enantioselective borylcupration of styrenes, followed by a highly selective direct addition to 1,3-diketones. The bicyclic scaffolds with three chiral carbon centers, including two tetrasubstituted carbons, were generated in excellent yields, diastereoselectivities, and enantioselectivities. This catalytic tandem reaction has great potential for further synthetic application of the chiral polycyclic compounds, because of the versatility of the functional groups in the products.

Investigating isoindoline, tetrahydroisoquinoline, and tetrahydrobenzazepine scaffolds for their sigma receptor binding properties

Substituted norbenzomorphans are known to display high affinity and selectivity for the two sigma receptor (σR) subtypes. In order to study the effects of simplifying the structures of these compounds, a scaffold hopping strategy was used to design severa

SIGMA RECEPTOR BINDERS

Provided herein, inter alia, are compounds and methods of treating diseases including cancer, neurological disease, alcohol withdrawal, depression and anxiety, traumatic brain injury, and neuropathic pain.