Enantiomerically enriched organoboron compounds are of considerable utility in organic synthesis. Unlike other organometallic reagents (e.g., RM, M = Li, Al, Mg, or Zn), boron‐containing hydrocarbons possess a number of desirable properties that include air, moisture, and configurational stability in addition to ease of preparation and exceptional functional group tolerance. Multicomponent, CB bond forming reactions, catalyzed by readily accessible, copper‐based complexes, have recently emerged as an attractive option for efficient, chemo‐, regio‐, diastereo‐ and enantioselective generation of multifunctional organoboron compounds. These processes typically begin with the addition of a copper–boryl complex to an alkenyl site, generating a copper–alkyl intermediate that then reacts with an electrophile. The focus of this chapter will be these transformations. A brief analysis of the key mechanistic nuances that impact the observed selectivity will be followed by an overview of the scope and limitations of the various strategies and their applications to the synthesis of bioactive molecules.
This study investigated the heat level rating of several varieties of Korean red peppers. The chemical constitution of Korean red pepper samples were as follows: 0.54∼290.15 mg% capsaicinoids, 79.22∼139.09 ASTA value, and 16.76∼29.92% free sugar content. The heat level of the Korean red pepper samples was evaluated by trained panelists and the correlation coefficient and F value (0.001%) of the panelist’s results were determined to be significant. In the principle component analysis (PCA), PC1 (capsaicinoids) and PC2 (free sugar) were shown to represent 31.98% and 25.77% of the total variance, respectively. The results of panelists trained for red pepper heat rating were evaluated using analysis of variance and correlation analysis. The trained panelists showed a high F value (p=0.05) and high correlation coefficient. A high correlation efficient of 0.84∼0.93 for the test samples with a 40 Scoville heat unit (32,000 SHU red pepper powder) was reported in the sensory evaluation of the Korean red pepper heat level by a trained panel. However, the panel showed a low correlation efficiency of 0.70 R2 when the 60 SHU test samples were included in the analysis.
Autophagy activation has the potential to ameliorate neurodegenerative disease phenotypes, including protein aggregation, lipid level perturbations and axonal trafficking defects. We performed a high content imaging-based screen assessing 940,000 small molecules to identify those that accelerate lipid droplet clearance. Hits were validated in diverse cell lines and by counter-screening. Of the 77 structurally diverse validated hits, 24 increase autophagy flux. Herein, we highlight CCT020312 as a mammalian target of rapamycin (mTOR) inhibitor-independent autophagy activator, which should function without compromising human immune function. CCT020312 dose-dependently reduces cytotoxic axonal mutant prion protein aggregate levels within endosomes of primary murine hippocampal neurons and normalizes axonal trafficking deficiencies. Moreover, CCT020312 robustly clears phosphorylated insoluble tau, while reducing tau-mediated neuronal stress vulnerability in patient-derived neuronal models. CCT020312 also restores lysosomal function in neurons differentiated from sporadic Alzheimer's patients' fibroblasts bearing epigenetic marks of aging. Taken together, we describe a promising strategy to uncover novel pharmacological agents that normalize cellular neurodegenerative disease pathology.
This study investigated the sensory attributes of Satsuma mandarins to provide basic data for the establishment of a quality grade establishment of mandarins. Samples of the mandarins in different sizes (small, medium, and large) were collected via organic green house cultivation, conventional cultivation without pesticides and conventional cultivation in Jeju Island. Eight trained panels performed the triplicate measurements. From the results of the quantitative descriptive analysis, mandarin samples were selected with five types of appearances (gloss intensity, color intensity, peel width, damage degree, and peel texture), three types of odors (sour, sweet, fresh), six types of tastes (sour, sweet, bitter, fresh, tasteless, and off flavor) four types of texture (hardness, granule toughness, juicy, and tough feel), and three types of after-tastes (sour, sweet, and bitter). The results of the analysis of the quality characteristics of the samples showed that their, pH, total acidity and solids contents differed depending on the size of the samples more than their cultivation methods. The correlation coefficients between the quality properties of the mandarins showed that their, sample size was positively correlated with their peel width and toughness. Moreover, the soluble solid of sample was positively correlated with its color intensity, sweet and fresh orange flavor. However, soluble solid content of the samples was negatively coreelated with their bitter flavor, tastelessness, and off flavor. In the principal component analysis of the sensory attributes data, PC1 represented the soluble solid, gross intensity, orange color, sour and sweet odor, unique mandarin flavor (sweet and, fresh orange), etc., and PC2 (26.77%) the size, pH, sample acidity, and peel texture.
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