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Abstract Using response surface methods, we have re-optimized a palladium-catalyzed method for coupling ClZn(pyrrolide) with aryl bromides to selectively generate 2-arylpyrroles. We optimized based on four variables: temperature, ClZn(pyrrolide)/ArBr ratio, catalyst loading, and time. To find a protocol applicable to most substrates of interest, we optimized three different substrates: a bulky arene (mesityl bromide), an electron-rich arene [4-(NMe2)C6H4Br], and an electron-deficient arene [3,5-(CF3)2C6H3Br]. The re-optimized procedures give as good or better yields than the previously published protocols, always in a fraction of the time. In addition, the reactions are generally cleaner with the new conditions, especially with electron-rich substrates, making the products easier to isolate. We applied the conditions to a variety of different substrates in each category, which provided good to excellent isolated yields. 

A room temperature stable Y(ii)bis(amide) has been prepared and fully characterized. The complex reacts withtert-butylisocyanide to make a rare example of a transition metal isocyanide, CN–Y(NHAr*)₂. 

Metal quinoline complexes were prepared using a quinoline-based proteasome inhibitor (Quin1) and an inactive quinoline ligand (Quin2), and their cytotoxicities are reported towards multiple myeloma-related cell lines. 

SAR on NRF2 inhibitor MSU38225 has led to a compound that inhibits expression of NRF2 target genes, reduces proliferation of lung cancer cells through G2/M arrest, and lowers cell migration. 

Treatment of isoxazoles with enamines leads to an inverse electron-demand hetero-Diels–Alder reaction that produces substituted pyridines in the presence of TiCl 4 (THF) 2 and titanium powder. The reaction is highly regioselective with only a single isomer of the product observed by GC/MS and tolerant of many common functional groups. The transformation was examined computationally, and it was found that TiCl 4 (or a similar Lewis acid) likely acts to catalyze the reaction. After the initial [4 + 2]-cycloaddition, the oxaza-[2.2.1]-bicycle produced likely ring opens before amine loss to give an N -oxide. The pyridine is then obtained after reduction with TiCl 4 and titanium powder.