Scalable Total Syntheses of (±)-Catellatolactams A and B

Org Lett. 2023 Feb 17;25(6):1003-1007. doi: 10.1021/acs.orglett.3c00132. Epub 2023 Feb 7.

Abstract

The first total syntheses of (±)-catellatolactams A and B, two novel ansamacrolactams, are described in 5 and 8 steps, respectively. The strategy relies on an amidation reaction to couple the acylated Meldrum's acid and an aryl amine, a regioselective C-H insertion to construct the γ-lactam moiety, and an RCM reaction to forge the macrocycles with E-olefin. This concise and scalable synthesis provided over 200 mg of the target molecules.