A novel series of optically active 2,6-disubstituted alkylphenols with improved anesthetic profiles compared to widely used propofol were synthesized. The incorporation of the cyclopropyl group not only increased the steric effect but also introduced stereoselective effects over their anesthetic properties. Compounds 1, 2, and 6 were selected as potential candidates for further preclinical development including studies of their water-soluble prodrugs. Clinical studies of candidate compound 6 (Haisco HSK3486) as a general anesthetic are being performed in Australia and China.
The first deacylative allylic C-H alkylation has been established by employing the palladium-catalyzed allylic C-H activation and decarboxylative nucleophile generation. A wide scope of nucleophiles are tolerated and densely functionalized alkylation products turn out to be furnished in moderate to good yield. More importantly, this strategy provides an alternative method for the allylic C-H alkylation with less stabilized carbon nucleophiles, and can be further expanded to the synthesis of unconjugated enynes.
3-Acyl imidazo[1,5-a]pyridines, featured pharmaceutical moieties that were prepared by a three-step reaction conventionally, could be obtained in one step by an electrochemical tandem sp 3 (C−H) double amination of acetophenones with pyridine ethylamines using ammonium iodide as a redox mediator.
Chemical plating has recently been employed for the preparation of flexible piezoresistive sensors; however, plating solutions and processes that affect the sensitivity still need further exploration. In the study, a sponge-based flexible sensor with copper as its conductive material is prepared using electroless plating. The variation in sponge resistance and sensitivity changes with different plating times are studied. It is found that, with the increasing plating time, the conductivity increases and the resistance of sample will decrease. Moreover, the range of resistance difference will decrease under compression, thus the sensitivity decreases. Furthermore, the sensor’s applications were assessed, verifying the practicability of the developed preparation method. This study may bring ideas for the new development of flexible pressure sensors.
The exposure of 365 nm light irradiation significantly accelerates the oxidase-mimicking activity of black phosphorus quantum dots, allowing sensitive colorimetric assay of acetylcholinesterase activity and evaluation of its inhibitor screening.
New cinchona‐based primary amine catalysts were prepared and screened as organocatalysts for the γ‐alkylation of α,β‐unsaturated aldehydes with bis(4‐dimethylaminophenyl)methanol. Catalyst C3 containing acetic acid group yielded γ‐alkylated products in good yields (up to 94 %) with up to 90 % ee. This new primary aminocatalyst provide new opportunities to explore novel asymmetric transformations.
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