A bis(amino)cyclopropenylidene-catalyzed direct method for the synthesis of α,α'-diarylated ketones from aromatic as well as heteroaromatic aldehydes has been developed. This unprecedented organocatalytic protocol offers access to a wide range of α,α'-diarylated ketones in moderate to excellent yields under mild conditions through umpolung of aldehydes followed by 1,6-conjugate addition with para-quinone methides.
A continuous‐flow homogeneous photocatalytic method has been devised for the direct arylation of 2H‐indazoles. This visible‐light‐promoted approach directly accesses a wide range of structurally diverse C3‐arylated scaffolds of biological interest in a fast (1 min), single‐step reaction by using eosin Y as an organophotocatalyst. Furthermore, a microreactor technology is also employed for the fast synthesis of liver X receptor inhibitor drugs with very good yields under metal‐free conditions, whereas the reported methods required multiple steps and much longer reaction times (18–24 h).
The organocatalytic behavior of N-heterocyclic carbenes in the aerobic oxidation of aromatic aldehydes to esters with boronic acids has been explored. This transition metal-free protocol allows access to a wide variety of aromatic esters in good to excellent yields under mild reaction conditions.
A highly chemoselective
intermolecular crossed acyloin condensation
between aromatic aldehydes and trifluoroacetaldehyde ethyl hemiacetal
has been developed under mild reaction conditions using N-heterocyclic carbene as a catalyst. A wide range of aromatic aldehydes
bearing electron-withdrawing and -donating substituents underwent
a smooth transformation to their corresponding trifluoromethyl containing
acyloin derivatives in moderate to good yields.
Continuous pharmaceutical manufacturing receives intense attention as an alternative way to meet flexible market needs with the assurance of higher safety and quality control.
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