207845-32-7

Upstream product

• 618-91-7 methyl 3-iodo-benzoate 
• 536-74-3 phenylacetylene 
• 618-89-3 methyl 3-bromobenzoate 
• 2170-06-1 1-Phenyl-2-(trimethylsilyl)acetylene 
• 2905-65-9 methyl 3-chlorobenzoate 
• 108-90-7 chlorobenzene 
• 115-19-5 2-methyl-but-3-yn-2-ol 
• 67-56-1 methanol 
• 3757-88-8 tributylstannylethynylbenzene 
• 618-51-9 3-Iodobenzoic acid 

Downstream Products

• 123926-88-5 [3-(2-phenylethynyl)phenyl]methanol 
• 93866-50-3 3-(2-phenylethynyl)benzoic acid 
• 194605-54-4 3-phenethylbenzoic acid methyl ester 
• 74070-40-9 [3-((Z)-Styryl)-phenyl]-methanol 

Relevant academic research and scientific papers

Palladium-catalyzed efficient and one-pot synthesis of diarylacetylenes from the reaction of aryl chlorides with 2-methyl-3-butyn-2-ol

An efficient and practical synthetic method has been developed for the preparation of symmetrical diarylacetylenes from the direct reaction of aryl chlorides with 2-methyl-3-butyn-2-ol catalyzed by palladium(II) chloride-bis(tricyclohexylphosphine) [PdCl2(PCy3) 2] under mild reaction conditions. Unsymmetrical diarylated acetylenes could be also obtained by using two different aryl chlorides simultaneously. The catalytic procedure includes a novel one-pot palladium-catalyzed, double Sonogashira coupling of inactivated aryl chlorides without use of copper(1) as co-catalyst.

Recyclable cellulose-palladium nanoparticles for clean cross-coupling chemistry

Cheap, recyclable, and robust cellulose-palladium nanoparticles were developed and fully characterized by FTIR, TEM, XPS, TGA, and NMR. The nanoparticles enabled cross-coupling chemistry in a truly general fashion i.e., Suzuki-Miyaura, Heck, Sonogashira, and C-H activation. Notably, all types of transformations were achieved with a single type of nanocatalyst. Complete recyclability of the catalyst and low traces of palladium in the product demonstrates the greenness of the protocol.

Recyclable Pd/CuFe2O4 nanowires: A highly active catalyst for C-C couplings and synthesis of benzofuran derivatives

Pd/CuFe2O4 nanowire-catalyzed cross coupling transformations are described. Notably, these reactions showed excellent functional group tolerance. Further, the protocol is applied to a one-pot synthesis of benzofurans via a Sonogashira coupling and intramolecular etherification sequence. The catalyst was reused and found to maintain its activity and stability.

Development of Dipeptidic hGPR54 Agonists

A series of dipeptides were designed as potential agonists of the human KiSS1-derived peptide receptor (hGPR54). While the sequence Arg-Trp-NH2was the most efficient in terms of affinity, we established a convergent synthetic strategy to optimi

HYDROXAMIC ACID DERIVATIVES AS GRAM-NEGATIVE ANTIBACTERIAL AGENTS

The invention relates to chemical compounds of formula (IB): or a salt thereof. In some embodiments, the invention relates to inhibitors of UDP-3-0 — (R-S-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC). In still further embodiments, the invention relates to pharmaceutical compositions comprising compounds disclosed herein and their use in the prevention and/or treatment of Gram- negative bacterial infections.

Efficient copper-catalyzed cross-coupling reaction of alkynes with aryl iodides

A copper-catalyzed cross-coupling reaction of alkynes with aryl iodides is described. The system, tolerates a broad range of functional groups and enables the use of sterically demanding substrates with only 1.0-2.5 mol-% of Cu 2O and 1.0-2.5 mol-% of xantphos as the catalyst.

Zinc chloride-promoted aryl bromide-alkyne cross-coupling reactions at room temperature

(Chemical Equation Presented) Substoichiometric amounts of ZnCl2 promote the room temperature, Pd/P(t-Bu)3-catalyzed cross-coupling of aryl bromides with alkynes. Pd(I) dimer 1 is demonstrated to be a particularly active precatalyst for this reaction. The reaction is general for a wide variety of aryl bromides.

Alpha-helical mimetics

Benzoyl urea derivatives that are alpha helical peptides mimetics that mimic BH3-only proteins, compositions containing them, their conjugation to cell-targeting-moieties, and their use in the regulation of cell death are disclosed. The benzoyl urea derivatives are capable of binding to and neutralizing pro-survival Bcl-2 proteins. Use of benzoyl urea derivatives in the treatment and/or prophylaxis of diseases or conditions associated with deregulation of cell death are also described.

Copper-free palladium-catalyzed sonogashira-type coupling of aryl halides and 1-aryl-2-(trimethylsilyl)acetylenes

A one-pot procedure for the direct coupling of 1-aryl-2- trimethylsilylacetylenes with aryl halides to give diaryl acetylenes is reported. The procedure does not involve the use of copper(I) iodide. Improvement in reaction yields has been obtained by replacing conventional oil bath heating with the use of microwave dielectric heating.

C17,20-lyase inhibitors I. Structure-based de novo design and SAR study of C17,20-lyase inhibitors.

Novel nonsteroidal C(17,20)-lyase inhibitors were synthesized using de novo design based on its substrate, 17 alpha-hydroxypregnenolone, and several compounds exhibited potent C(17,20)-lyase inhibition. However, in vivo activities were found to be short-lasting, and in order to improve the duration of action, a series of benzothiophene derivatives were evaluated. As a result, compounds 9h, (S)-9i, and 9k with nanomolar enzyme inhibition (IC(50)=4-9 nM) and 9e (IC(50)=27 nM) were identified to have powerful in vivo efficacy with extended duration of action. The key structural determinants for the in vivo efficacy were demonstrated to be the 5-fluoro group on the benzothiophene ring and the 4-imidazolyl moiety. Superimposition of 9k and 17 alpha-hydroxypregnenolone demonstrated their structural similarity and enabled rationalization of the pharmacological results. In addition, selected compounds were also identified to be potent inhibitors of human enzyme with IC(50) values of 20-30 nM.