Coumarin derivatives are essential scaffolds in medicinal and synthetic chemistry. Compounds of this class have shown important activities, such as anticancer and antiparasitic, besides the commercially available drugs. These properties led to the development of efficient and greener synthetic methods to achieve the 2H-chromen-2-one core. In this context, the advances in asymmetric organocatalyzed synthesis of coumarin derivatives are discussed in this review, according to the mode of activation of the catalyst.
Quinazoline derivatives draw attention from a synthetic and medicinal chemistry point of view, given the wide range of biological activities already described. This class of fused Nheterocyclic compounds has also shown its importance and potential pharmacological application. This Review covers the contributions reported in the last ten years for the synthesis of pyrroloquinazoline derivatives, focusing on greener protocols to obtain these adducts, such as multicomponent reactions, photocatalysis, microwaves, electrosynthesis among others.
A simple procedure for the copper‐catalyzed synthesis of 3‐(N‐heteroaryl)acrylonitriles was developed. Using a combination of Lewis and Brønsted acids, this one‐pot procedure undergoes via a radical conjugated addition and dehydration processes, without isolation of any intermediate, affording the acrylonitriles. This diastereoselective approach allowed the synthesis of a broad scope of quinazoline derivatives (22 examples) with moderate to good yields and good functional‐group tolerance and could be extended to other N‐heterocyles such as quinolines and isoquinolines. Based on control experiments, a mechanistic proposal for this new transformation is also presented.
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