81787-62-4

Upstream product

• 75-77-4 chloro-trimethyl-silane 
• 456-61-1 (2,2-Dichloro-1,1-difluoroethoxy)benzene 
• 93782-13-9 β,β-dibromo-o-(trimethylsilyloxy)styrene 
• 108-95-2 phenol 
• 95-56-7 2-hydroxybromobenzene 
• 1066-54-2 trimethylsilylacetylene 
• 533-58-4 2-Iodophenol 
• 59214-70-9 3-bromobenzofuran 
• 864908-76-9 2-iodophenyl isopropylcarbamate 
• 17614-10-7 phenyl N-isopropylcarbamate 

Downstream Products

• 132932-61-7 2-(p-acetylphenyl)benzofuran 
• 211696-94-5 2-(trimethylsilylethynyl)-(2-propenyloxy)benzene 
• 835596-43-5 o-[(2E,4)-pentadienyloxy](trimethylsilylethynyl)benzene 
• 63157-19-7 (1-benzofuran-2-yl)(4-methoxyphenyl)methanone 
• 118-93-4 o-hydroxyacetophenone 
• 77038-49-4 (±)-2-(2-naphthyl)chromanone 
• 1111079-09-4 (E)-3-cyclohexyl-1-(2-hydroxyphenyl)prop-2-en-1-one 
• 1608125-86-5 bis(2-((trimethylsilyl)ethynyl)phenyl) fumarate 

Relevant academic research and scientific papers

ANTIBACTERIAL ADJUVANTS AND APPLICATIONS THEREOF

In one aspect, compounds and methods are described herein for treating gram negative bacteria having resistance to cationic antimicrobial peptides. In some embodiments, for example, compounds of formula I are provided. In another aspect, a treatment for a gram negative bacterial infection comprises a cationic antimicrobial protein (CAP) in conjunction with a compound of formula I.

An Iron-Mesoionic Carbene Complex for Catalytic Intramolecular C-H Amination Utilizing Organic Azides

The synthesis of N-heterocycles is of paramount importance for the pharmaceutical industry. They are often synthesized through atom economic and environmentally unfriendly methods, generating significant waste. A less explored, but greener, alternative is

Selective Rhodium-Catalyzed Hydroformylation of Terminal Arylalkynes and Conjugated Enynes to (Poly)enals Enabled by a π-Acceptor Biphosphoramidite Ligand

The hydroformylation of terminal arylalkynes and enynes offers a straightforward synthetic route to the valuable (poly)enals. However, the hydroformylation of terminal alkynes has remained a long-standing challenge. Herein, an efficient and selective Rh-catalyzed hydroformylation of terminal arylalkynes and conjugated enynes has been achieved by using a new stable biphosphoramidite ligand with strong π-acceptor capacity, which affords various important E-(poly)enals in good yields with excellent chemo- and regioselectivity at low temperatures and low syngas pressures.

Biomimetic carbene cascades enabled imine derivative migration from carbene -bearing thiocarbamates

Inspired by the body circulation of Omeprazole (irreversible proton pump inhibitor), we disclose the carbene-triggered cascades for the synthesis of 2-aminobenzofuran derivatives from N-sulfonyl-1,2,3-triazoles or benzothioazole-bearing thiocarbamates, which represents an unprecedented imine derivative migration process. Furthermore, the desulfurizing reagent-free Barton-Kellogg-type reactions starting from N-sulfonyl-1,2,3-triazoles have also been achieved for the first time, and elemental sulfur is confirmed as a byproduct during this transformation. Both experimental data and DFT calculations further thoroughly explained the unique reactivity.

A Facile Construction of Bisheterocyclic Methane Scaffolds through Palladium-Catalyzed Domino Cyclization

A convenient palladium-catalyzed domino cyclization reaction for the construction of bis(benzofuranyl)methane scaffolds bearing an all-carbon quaternary center has been described. In the cascade process, one C(sp2)—O bond, two C(sp2)—C(sp3) bonds as well as two benzofuran rings are formed in a single synthetic sequence. The approach shows wide scope of substrates and good functional-group tolerance. Moreover, this methodology is successfully extended to the synthesis of benzofuranyl methyl chromane derivatives.

Photocatalytic Biheterocyclization of 1,7-Diynes for Accessing Skeletally Diverse Tricyclic 2-Pyranones

A new and green route to skeletally diverse oxo-heterocyclic architectures such as pyrano[3,4-c]chromen-2-ones and pyrano[3,4-c]quinolin-2-ones is reported via an unprecedented photocatalytic Kharasch-type cyclization/1,5-(SN″)-substitution/elimination/6π

Discovery of Novel UDP- N-Acetylglucosamine Acyltransferase (LpxA) Inhibitors with Activity against Pseudomonas aeruginosa

This study describes a novel series of UDP-N-acetylglucosamine acyltransferase (LpxA) inhibitors that was identified through affinity-mediated selection from a DNA-encoded compound library. The original hit was a selective inhibitor of Pseudomonas aeruginosa LpxA with no activity against Escherichia coli LpxA. The biochemical potency of the series was optimized through an X-ray crystallography-supported medicinal chemistry program, resulting in compounds with nanomolar activity against P. aeruginosa LpxA (best half-maximal inhibitory concentration (IC50) 20 μM and MIC > 128 μg/mL). The mode of action of analogues was confirmed through genetic analyses. As expected, compounds were active against multidrug-resistant isolates. Further optimization of pharmacokinetics is needed before efficacy studies in mouse infection models can be attempted. To our knowledge, this is the first reported LpxA inhibitor series with selective activity against P. aeruginosa.

Thermal [2 + 2]-cycloaddition between silylalkynes and allenylphenols followed by the nucleophilic addition of water: Metal-free and economical synthesis of arylcyclobutenals

Herein, we report an unprecedented thermal [2 + 2]-cycloaddition between silylalkynes and allenylphenols to form an aromatizing cyclobutachromene intermediate, followed by the nucleophilic addition of water to yield functionalized arylcyclobutenals. This reaction is atom- and pot-economical because all the atoms contained in the starting material are retained in the final product, no other reactants are required, and it proceeds in one-pot.

Rhenium-Catalyzed Intramolecular Carboalkoxylation and Carboamination of Alkynes for the Synthesis of C3-Substituted Benzofurans and Indoles

A rhenium-catalyzed carboalkoxylation and carboamination of alkyne is reported. This reaction provides an efficient route to synthesize de novo C3-substituted benzofurans and indoles under mild conditions in moderate to good yields. Mechanistic studies re

Oxyacylation of Iodoalkynes: Gold(I)-Catalyzed Expeditious Access to Benzofurans

(Acetonitrile)[1,3-bis(2,6-diisopropylphenyl)-imidazole-2-ylidene] gold(I) catalyzes the cycloisomerization of 2-(iodoethynyl)aryl esters to give 3-iodo-2-acyl benzofurans. This catalytic transformation is the result of an unprecedented selective syntheti