This review describes the research progress of the N‐formylsaccharin as a newly efficient and environmentally friendly carbon monoxide (CO) surrogate in the carbonylation reactions including the synthesis of aldehydes, esters, ketones, acyl fluorides or other reactions. Besides, its advantages in term of inexpensive, ease of handling and stable on storage significantly enhance practicality of the approach in laboratory scale.

The carbonylative Sonogashira coupling reaction of aromatic bromide with terminal alkynes has been developed with N‐formylsaccharin as a CO source. The reaction, which has certain advantages in cost and safety of raw materials, is carried out in a simple and safe one‐pot method. A variety of alkynones with good functional group compatibility can be obtained in medium to high yields.

Background: Curcumin is a polyphenol compound with highly pharmacological activities extracted from plant turmeric. The clinical application of curcumin is limited due to the shortcomings of poor water solubility, instability, and low bioavailability. Objective: Modifying the 4', 4''-bit of curcumin is an effective strategy to improve the pharmacological activity of curcumin. Conclusion: In this review, we focused on the strategy of synthesis, medicinal properties, and structure-function relationship of 4', 4''-bit modified curcumin derivatives.