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An efficient transition-metal-free protocol for the hydroboration of aldehydes and ketones (reduction) was developed. The hydroboration of a wide range of aldehydes and ketones with pinacolborane (HBpin) under the K2CO3 catalyst has been studied. The reaction system is practical and reliable and proceeds under extremely mild and operationally simple conditions. No prior preparation of the complex metal catalyst was required, and hydroboration occurred stoichiometrically. Further, the chemoselective reduction of aldehydes over ketones was carried out. Moreover, we demonstrated the use of K2CO3 as an efficient catalyst for the hydroboration of alkenes. The operational simplicity, inexpensive and transition-metal-free catalyst, and the applicability to gram-scale synthesis strengthen its potential applications for hydroboration (reduction) at an industrial scale.

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Pyruvate dehydrogenase kinase 4 (PDK4) activation is associated with metabolic diseases including hyperglycemia, insulin resistance, allergies, and cancer. Structural modifications of hit anthraquinone led to the identification of a new series of allosteric PDK4 inhibitors. Among this series, compound 8c showed promising in vitro activity with an IC 50 value of 84 nM. Good metabolic stability, pharmacokinetic profiles, and possible metabolites were suggested. Compound 8c improved glucose tolerance in diet-induced obese mice and ameliorated allergic reactions in a passive cutaneous anaphylaxis mouse model. Additionally, compound 8c exhibited anticancer activity by controlling cell proliferation, transformation, and apoptosis. From the molecular docking studies, compound 8c displayed optimal fitting in the lipoamide binding site (allosteric) with a full fitness, providing a new scaffold for drug development toward PDK4 inhibitors.