309757-75-3

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 1866-38-2 m-Chlorocinnamic acid 
• 27784-76-5 tert-butyl diethylphosphonoacetate 
• 587-04-2 m-Chlorobenzaldehyde 
• 1663-39-4 tert-Butyl acrylate 
• 63503-60-6 3-chlorophenylboronic acid 
• 625-99-0 3-iodochlorobenzene 
• 456-39-3 3-chlorobenzenediazonium tetrafluoroborate 

Relevant academic research and scientific papers

Gelatin-pyrolyzed mesoporous N-doped carbon supported Pd as high-performance catalysts for aqueous Heck reactions

Nitrogen-doped mesoporous carbon-supported Pd (Pd@N-C) catalysts were prepared by pyrolyzing gelatin/templates/PdCl2 hydrogels under N2 atmosphere at 800°C. Using poly (ethylene glycol) block poly (propylene glycol) block poly (ethyl

Ligand-free PdCl2-catalyzed heck reaction of arylboronic acids and olefins under reusable TBAB/H2O conditions

A novel method was developed for Heck reaction of olefins and arylboronic acids using a ligand-free PdCl2 catalyst to afford the coupling products with excellent regio- and stereoselectivity. It is noteworthy that the PdCl2/CuSO4/K2CO3/TBAB/H 2O system can be recovered and used for three cycles directly. Georg Thieme Verlag Stuttgart, New York.

Heck-Matsuda reactions catalyzed by a hydroxyalkyl-functionalized NHC and palladium acetate

The functionalized NHC obtained from salt 2 is a good ligand for palladium in the Heck-Matsuda reaction of arenediazonium salts and different alkenes. The reaction is performed with low catalyst loading (0.5-1 mol-% of Pd) and in the absence of a base for acrylates. The protocol is also useful for the preparation of cinnamide derivatives. Compound U-77863 has been prepared successfully in good isolated yield. Cyclohexene was found to be an appropriate substrate for the reaction, giving the corresponding 1-arylcyclohexene as a single regioisomer under the studied reaction conditions. The optimal parameters of the reaction were studied by employing a design of experiments approach. Thus, the use of a small set of reactions allows the trends of the different factors to be studied. This study revealed that the best catalytic system is formed by combination of Pd(OAc)2 and salt 2 in a 1:2 ratio. This catalytic system produces better results without the use of a base. Copyright

Arylcyclopropanecarboxyl guanidines as novel, potent, and selective inhibitors of the sodium hydrogen exchanger isoform-1

A novel series of arylcyclopropanecarboxyl guanidines was synthesized and evaluated for activity against the sodium hydrogen exchanger isoform-1 (NHE-1). In biological assays conducted in an AP1 cell line expressing the human NHE-1 isoform, the starting cyclopropane 3a (IC50 = 3.5 μM) shows inhibitory activity comparable to cariporide (IC50 = 3.4 μM). Structure-activity relationships are used to optimize the affinity of various acyl guanidines for NHE-1 by screening the effect of substituents at both aryl and cyclopropyl rings. It is demonstrated that introduction of appropriate hydrophobic groups at the phenyl ring and a gem-dimethyl group at the cyclopropane ring enhances the NHE-1 inhibitory activity by up to 3 orders of magnitude (compound 7f, IC50 = 0.003 μM). In addition, the gem-dimethyl series of analogues seem to display improved oral bioavailability and longer plasma half-life in rats. Furthermore, the lead benzodihydrofuranyl analogue 1 (BMS-284640) shows over 380-fold increased NHE-1 inhibitory activity as well as improved selectivity for NHE-1 over NHE-2 compared to cariporide.

Asymmetric synthesis of β-haloaryl β-amino acid derivatives

Lithium N-benzyl-N-α-methyl-4-methoxybenzylamide may be employed as a homochiral ammonia equivalent for the synthesis of homochiral β-haloaryl β-amino acid derivatives via a strategy involving its conjugate addition to α,β-unsaturated β-haloaryl acceptors and subsequent oxidative deprotection with ceric ammonium nitrate.