A Review of the Pharmacological Activities and Recent Synthetic Advances of γ-Butyrolactones

• Published in: International journal of molecular sciences Vol. 22; no. 5; p. 2769
• Main Authors: Hur, Joonseong, Jang, Jaebong, Sim, Jaehoon
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI 09.03.2021; MDPI AG
• Subjects: 4-Butyrolactone - chemical synthesis; 4-Butyrolactone - chemistry; 4-Butyrolactone - pharmacology; Animals; Green Chemistry Technology; Humans; lactone synthesis; lactonization; Molecular Structure; pharmacological activities; recent advances; Review; γ-butyrolactone; pharmacological activities; lactonization; γ-butyrolactone; lactone synthesis; recent advances
• ISSN: 1422-0067; 1661-6596; 1422-0067
• DOI: 10.3390/ijms22052769

-Butyrolactone, a five-membered lactone moiety, is one of the privileged structures of diverse natural products and biologically active small molecules. Because of their broad spectrum of biological and pharmacological activities, synthetic methods for -butyrolactones have received significant attention from synthetic and medicinal chemists for decades. Recently, new developments and improvements in traditional methods have been reported by considering synthetic efficiency, feasibility, and green chemistry. In this review, the pharmacological activities of natural and synthetic -butyrolactones are described, including their structures and bioassay methods. Mainly, we summarize recent advances, occurring during the past decade, in the construction of -butyrolactone classified based on the bond formation in -butyrolactone between (i) C5-O1 bond, (ii) C4-C5 and C2-O1 bonds, (iii) C3-C4 and C2-O1 bonds, (iv) C3-C4 and C5-O1 bonds, (v) C2-C3 and C2-O1 bonds, (vi) C3-C4 bond, and (vii) C2-O1 bond. In addition, the application to the total synthesis of natural products bearing -butyrolactone scaffolds is described.